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Chemistry

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Also known as: Femring, Femtrace, Estradiol 3-acetate, Estradiol-3-acetate, 4245-41-4, Estradiol acetate [usan]
Molecular Formula
C20H26O3
Molecular Weight
314.4  g/mol
InChI Key
FHXBMXJMKMWVRG-SLHNCBLASA-N
FDA UNII
5R97F5H93P

Estradiol Acetate
Estradiol Acetate is the acetate salt form of estradiol, the most potent, naturally produced estrogen. Estradiol acetate diffuses through the cell membrane and binds to and subsequently activates the nuclear estrogen receptor found in the reproductive tract, breast, pituitary, hypothalamus, liver, and bone. The activated complex binds to the estrogen response element on the DNA and activates the transcription of genes involved in the functioning of the female reproductive system and secondary sex characteristics.
1 2D Structure

Estradiol Acetate

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
[(8R,9S,13S,14S,17S)-17-hydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-3-yl] acetate
2.1.2 InChI
InChI=1S/C20H26O3/c1-12(21)23-14-4-6-15-13(11-14)3-5-17-16(15)9-10-20(2)18(17)7-8-19(20)22/h4,6,11,16-19,22H,3,5,7-10H2,1-2H3/t16-,17-,18+,19+,20+/m1/s1
2.1.3 InChI Key
FHXBMXJMKMWVRG-SLHNCBLASA-N
2.1.4 Canonical SMILES
CC(=O)OC1=CC2=C(C=C1)C3CCC4(C(C3CC2)CCC4O)C
2.1.5 Isomeric SMILES
CC(=O)OC1=CC2=C(C=C1)[C@H]3CC[C@]4([C@H]([C@@H]3CC2)CC[C@@H]4O)C
2.2 Other Identifiers
2.2.1 UNII
5R97F5H93P
2.3 Synonyms
2.3.1 Depositor-Supplied Synonyms

1. Femring

2. Femtrace

3. Estradiol 3-acetate

4. Estradiol-3-acetate

5. 4245-41-4

6. Estradiol Acetate [usan]

7. E3a

8. 5r97f5h93p

9. Estradiol Acetate (usan)

10. Dsstox_cid_25867

11. Dsstox_rid_81186

12. Dsstox_gsid_45867

13. [(8r,9s,13s,14s,17s)-17-hydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-3-yl] Acetate

14. Menoring

15. Cas-4245-41-4

16. 3-o-acetylestradiol

17. Estradiol, 3-acetate

18. 17beta-estradiol 3-acetate

19. Unii-5r97f5h93p

20. E 3a

21. Estradiol-acetate

22. Femring (tn)

23. 3-acetoxyestra-1,3,5(10)-trien-17beta-ol

24. 17beta-hydroxy-3-acetoxyestra-1,3,5(10)-triene

25. Schembl148561

26. Estra-1,3,5(10)-triene-3,17beta-diyl 3-acetate

27. Chembl1200430

28. Dtxsid7045867

29. Estradiol Acetate [vandf]

30. Chebi:135981

31. Estradiol 3-acetate [mi]

32. Estradiol Acetate [mart.]

33. Estradiol Acetate [who-dd]

34. Tox21_111359

35. Tox21_113661

36. Db13952

37. Estradiol Acetate [orange Book]

38. Ncgc00249885-01

39. D04061

40. 3-acetoxy-oestra-1,3,5(10)-trien-17beta-ol

41. 17beta-hydroxyestra-1,3,5(10)-trien-3-yl Acetate

42. 3-(acetyloxy)estra-1,3,5(10)-trien-17.beta.-ol

43. Q27262772

44. 17.beta.-hydroxyestra-1,3,5(10)-trien-3-yl Acetate

45. Estra-1,3,5(10)-triene-3,17-diol, (17beta)-, 3-acetate

46. Estra-1,3,5(10)-triene-3,17-diol, (17 Beta)-, 3-acetate

47. Estra-1,3,5(10)-triene-3,17-diol, (17.beta.)-, 3-acetate

2.4 Create Date
2006-10-25
3 Chemical and Physical Properties
Molecular Weight 314.4 g/mol
Molecular Formula C20H26O3
XLogP32.8
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count3
Rotatable Bond Count2
Exact Mass314.18819469 g/mol
Monoisotopic Mass314.18819469 g/mol
Topological Polar Surface Area46.5 Ų
Heavy Atom Count23
Formal Charge0
Complexity476
Isotope Atom Count0
Defined Atom Stereocenter Count5
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Indication

Femring is indicated for the treatment of vasomotor and urogenital symptoms associated with menopause. Use of Femring (estradiol acetate) has been shown to improve symptoms caused by atrophy of the vagina (such as dryness, burning, pruritus and dyspareunia) and/or the lower urinary tract (urinary urgency and dysuria).


FDA Label


5 Pharmacology and Biochemistry
5.1 Pharmacology

Estrogen mediates its effects across the body through potent agonism of the Estrogen Receptor (ER), which is located in various tissues including in the breasts, uterus, ovaries, skin, prostate, bone, fat, and brain. Estradiol binds to both subtypes of the Estrogen Receptor: Estrogen Receptor Alpha (ER) and Estrogen Receptor Beta (ER). Estradiol also acts as a potent agonist of G Protein-coupled Estrogen Receptor (GPER), which has recently been recognized as a major mediator of estradiol's rapid cellular effects.


5.2 FDA Pharmacological Classification
5.2.1 Pharmacological Classes
Estrogen Receptor Agonists [MoA]; Estrogen [EPC]; Estradiol Congeners [CS]
5.3 Absorption, Distribution and Excretion

Absorption

Drug delivery from Femring is rapid for the first hour and then declines to a relatively constant rate for the remainder of the 3-month dosing interval. Estradiol acetate is rapidly hydrolyzed to estradiol which is absorbed through the vaginal mucosa as evidenced by the mean time to maximum concentration (tmax) for estradiol of about 1 hour (range 0.25 to 1.5 hrs). Following the maximum concentration (Cmax=1129pg/mL), serum estradiol decreases rapidly such that by 24 to 48 hours postdose, serum estradiol concentrations are relatively constant through the end of the 3-month dosing interval.


Route of Elimination

Estradiol, estrone and estriol are excreted in the urine along with glucuronide and sulfate conjugates.


Volume of Distribution

The distribution of exogenous estrogens is similar to that of endogenous estrogens. Estrogens are widely distributed in the body and are generally found in higher concentrations in the sex hormone target organs.


5.4 Metabolism/Metabolites

Exogenous estrogens are metabolized using the same mechanism as endogenous estrogens. Estradiol is converted reversibly to estrone, and both can be converted to estriol, which is the major urinary metabolite. Estrogens also undergo enterohepatic recirculation via sulfate and glucuronide conjugation in the liver, biliary secretion of conjugates into the intestine, and hydrolysis in the gut followed by reabsorption. In postmenopausal women, a significant proportion of the circulating estrogens exist as sulfate conjugates, especially estrone sulfate, which serves as a circulating reservoir for the formation of more active estrogens.


Estradiol acetate has known human metabolites that include 6-[(3-acetyloxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl)oxy]-3,4,5-trihydroxyoxane-2-carboxylic acid.

S73 | METXBIODB | Metabolite Reaction Database from BioTransformer | DOI:10.5281/zenodo.4056560


5.5 Mechanism of Action

Estradiol enters target cells freely (e.g., female organs, breasts, hypothalamus, pituitary) and interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary. Increases in the down-stream effects of ER binding reverses some of the symptoms of menopause, which are primarily caused by a loss of estrogenic activity.


NDC API

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ESTRADIOL ACETATE

NDC Package Code : 64918-0105

Start Marketing Date : 2015-10-19

End Marketing Date : 2026-12-31

Dosage Form (Strength) : POWDER (1kg/kg)

Marketing Category : BULK INGREDIENT

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Virtual BoothSymbiotec: Global API manufacturer, specializing in Cortico-Steroids & Steroid-Hormone APIs.

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Estradiol Acetate

About the Company : Symbiotec, based in Indore, India, is a leading API manufacturer specializing in cortico-steroids and steroid-hormone APIs since 1995. Focused on R&D, sustainability, and innovatio...

Symbiotec, based in Indore, India, is a leading API manufacturer specializing in cortico-steroids and steroid-hormone APIs since 1995. Focused on R&D, sustainability, and innovation, it operates a state-of-the-art facility inaugurated in 2004. Certified by WHO-GMP, ISO, US FDA, and EU GMP, Symbiotec is a trusted provider known for quality, adaptability, efficiency, and competitive pricing in global healthcare. Note: Product(s) under patent(s) are offered only for R&D purposes as per the Patent Act & not for commercial sale.
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Fareva

Luxembourg
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Virtual BoothFareva: One stop for innovative drug development, precision manufacturing and high-quality APIs.

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Estradiol Acetate

About the Company : Founded in 1990 in France, Fareva is a global subcontractor providing R&D, production, and packaging services across pharmaceutical, cosmetics, and industrial sectors. Operating in...

Founded in 1990 in France, Fareva is a global subcontractor providing R&D, production, and packaging services across pharmaceutical, cosmetics, and industrial sectors. Operating in 13 countries with 41 sites and 13,000+ employees, Fareva manufactures and packages products including sterile injectables, biological drugs, conventional formulations, medical devices, and food supplements. The company also produces APIs at three sites, covering highly potent, sterile, cytotoxic, hormonal, and steroid APIs. Note: Product(s) under patent(s) are offered only for R&D purposes as per the Patent Act & not for commercial sale.
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Minakem

France
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Virtual BoothMinakem delivers API, HPAPI, steroids & CDMO services for generics with FDA/GMP certification, regulatory know-how & proven success.

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Estradiol Acetate

About the Company : MINAKEM is a cGMP custom manufacturer specializing in small molecule APIs, HPAPIs, and steroids. Its highly skilled R&D teams, supported by strong analytical and regulatory service...

MINAKEM is a cGMP custom manufacturer specializing in small molecule APIs, HPAPIs, and steroids. Its highly skilled R&D teams, supported by strong analytical and regulatory services, excel in process development and organic synthesis, operating under secrecy agreements to protect client IP. With three European and one Canadian production site, MINAKEM supports strategic sourcing and reshoring projects. Recently launched commercial generic APIs include Apixaban, Mirabegron, Fulvestrant, remifentanil, and esmolol. Note: Product(s) under patent(s) are offered only for R&D purposes as per the Patent Act & not for commercial sale.
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Virtual BoothAndrost Biotech delivering high-quality hormone APIs and intermediates with trusted global compliance and competitive excellence.

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Estradiol Acetate

About the Company : Androst Biotech India Private Limited (ABIPL) is a fast-growing manufacturer of Active Pharmaceutical Ingredients and intermediates, specializing in high-volume hormone production....

Androst Biotech India Private Limited (ABIPL) is a fast-growing manufacturer of Active Pharmaceutical Ingredients and intermediates, specializing in high-volume hormone production. Our FDA- and GMP-certified facility operates with strong quality systems, robust documentation support (COA, MSDS, DMF), and continuous R&D focus. Serving domestic and global markets, ABIPL delivers reliable, high-quality APIs at competitive prices, earning trust across an expanding international customer base. Note: Product(s) under patent(s) are offered only for R&D purposes as per the Patent Act & not for commercial sale.
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Virtual BoothGonane has API manufacturing expertise in new-age Corticosteroids, Hormones and other pharma raw materials.

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Estradiol Acetate

About the Company : Gonane Pharma is a contract pharmaceutical company based in Gujarat, India, specializing in the manufacturing and marketing of corticosteroids, hormones, antivirals, and oncology p...

Gonane Pharma is a contract pharmaceutical company based in Gujarat, India, specializing in the manufacturing and marketing of corticosteroids, hormones, antivirals, and oncology products. The company is supported by a dedicated team and promoters with over 25 years of experience in manufacturing, product promotion, and regulatory audits across markets including the EU, Mexico, China, Korea, and Russia. Gonane Pharma is also engaged with Japanese customers and continues to expand into new markets. Note: Product(s) under patent(s) are offered only for R&D purposes as per the Patent Act & not for commercial sale.
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Drugs in Development

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Details:

Estradiol Acetate is a Other Small Molecule drug candidate, which is currently being evaluated in phase III clinical studies for the treatment of undefined medical condition.


Lead Product(s): Estradiol Acetate,Inapplicable

Therapeutic Area: Undisclosed Brand Name: Undisclosed

Study Phase: Phase IIIProduct Type: Miscellaneous

Sponsor: Undisclosed

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable February 18, 2010

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Details : Estradiol Acetate is a Other Small Molecule drug candidate, which is currently being evaluated in phase III clinical studies for the treatment of undefined medical condition.

Product Name : Undisclosed

Product Type : Miscellaneous

Upfront Cash : Inapplicable

February 18, 2010

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FDF Dossiers

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ESTRADIOL ACETATE

Brand Name : FEMTRACE

Dosage Form : TABLET;ORAL

Dosage Strength : 0.45MG

Packaging :

Approval Date : 2004-08-20

Application Number : 21633

Regulatory Info : DISCN

Registration Country : USA

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ESTRADIOL ACETATE

Brand Name : FEMTRACE

Dosage Form : TABLET;ORAL

Dosage Strength : 0.9MG

Packaging :

Approval Date : 2004-08-20

Application Number : 21633

Regulatory Info : DISCN

Registration Country : USA

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Brand Name : FEMTRACE

Dosage Form : TABLET;ORAL

Dosage Strength : 1.8MG

Packaging :

Approval Date : 2004-08-20

Application Number : 21633

Regulatory Info : DISCN

Registration Country : USA

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ESTRADIOL ACETATE

Brand Name : FEMRING

Dosage Form : INSERT, EXTENDED RELEASE;VAGINAL

Dosage Strength : EQ 0.05MG BASE/24HR

Packaging :

Approval Date : 2003-03-20

Application Number : 21367

Regulatory Info : RX

Registration Country : USA

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ESTRADIOL ACETATE

Brand Name : FEMRING

Dosage Form : INSERT, EXTENDED RELEASE;VAGINAL

Dosage Strength : EQ 0.1MG BASE/24HR

Packaging :

Approval Date : 2003-03-20

Application Number : 21367

Regulatory Info : RX

Registration Country : USA

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FDA Orange Book

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ESTRADIOL ACETATE

Brand Name : FEMTRACE

Dosage Form : TABLET;ORAL

Dosage Strength : 0.45MG

Approval Date : 2004-08-20

Application Number : 21633

RX/OTC/DISCN : DISCN

RLD : Yes

TE Code :

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ESTRADIOL ACETATE

Brand Name : FEMTRACE

Dosage Form : TABLET;ORAL

Dosage Strength : 0.9MG

Approval Date : 2004-08-20

Application Number : 21633

RX/OTC/DISCN : DISCN

RLD : Yes

TE Code :

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APIL

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APIL

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ESTRADIOL ACETATE

Brand Name : FEMTRACE

Dosage Form : TABLET;ORAL

Dosage Strength : 1.8MG

Approval Date : 2004-08-20

Application Number : 21633

RX/OTC/DISCN : DISCN

RLD : Yes

TE Code :

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ESTRADIOL ACETATE

Brand Name : FEMRING

Dosage Form : INSERT, EXTENDED RELEASE;VAGINAL

Dosage Strength : EQ 0.05MG BASE/24HR

Approval Date : 2003-03-20

Application Number : 21367

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

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ESTRADIOL ACETATE

Brand Name : FEMRING

Dosage Form : INSERT, EXTENDED RELEASE;VAGINAL

Dosage Strength : EQ 0.1MG BASE/24HR

Approval Date : 2003-03-20

Application Number : 21367

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

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DOSAGE - INSERT, EXTENDED RELEASE;VAGINAL - E...DOSAGE - INSERT, EXTENDED RELEASE;VAGINAL - EQ 0.05MG BASE/24HR

USFDA APPLICATION NUMBER - 21367

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DOSAGE - INSERT, EXTENDED RELEASE;VAGINAL - E...DOSAGE - INSERT, EXTENDED RELEASE;VAGINAL - EQ 0.1MG BASE/24HR

USFDA APPLICATION NUMBER - 21367

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ABOUT THIS PAGE

Looking for 4245-41-4 / Estradiol Acetate API manufacturers, exporters & distributors?

Estradiol Acetate manufacturers, exporters & distributors 1

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PharmaCompass offers a list of Estradiol Acetate API manufacturers, exporters & distributors, which can be sorted by GMP, USDMF, JDMF, KDMF, CEP (COS), WC, Price,and more, enabling you to easily find the right Estradiol Acetate manufacturer or Estradiol Acetate supplier for your needs.

Send us enquiries for free, and we will assist you in establishing a direct connection with your preferred Estradiol Acetate manufacturer or Estradiol Acetate supplier.

PharmaCompass also assists you with knowing the Estradiol Acetate API Price utilized in the formulation of products. Estradiol Acetate API Price is not always fixed or binding as the Estradiol Acetate Price is obtained through a variety of data sources. The Estradiol Acetate Price can also vary due to multiple factors, including market conditions, regulatory modifications, or negotiated pricing deals.

API | Excipient name

Estradiol Acetate

Synonyms

Femring, Femtrace, Estradiol 3-acetate, Estradiol-3-acetate, 4245-41-4, Estradiol acetate [usan]

Cas Number

4245-41-4

Unique Ingredient Identifier (UNII)

5R97F5H93P

About Estradiol Acetate

Estradiol Acetate is the acetate salt form of estradiol, the most potent, naturally produced estrogen. Estradiol acetate diffuses through the cell membrane and binds to and subsequently activates the nuclear estrogen receptor found in the reproductive tract, breast, pituitary, hypothalamus, liver, and bone. The activated complex binds to the estrogen response element on the DNA and activates the transcription of genes involved in the functioning of the female reproductive system and secondary sex characteristics.

Estradiol Acetate Manufacturers

A Estradiol Acetate manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Estradiol Acetate, including repackagers and relabelers. The FDA regulates Estradiol Acetate manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Estradiol Acetate API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.

click here to find a list of Estradiol Acetate manufacturers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PhamaCompass.

Estradiol Acetate Suppliers

A Estradiol Acetate supplier is an individual or a company that provides Estradiol Acetate active pharmaceutical ingredient (API) or Estradiol Acetate finished formulations upon request. The Estradiol Acetate suppliers may include Estradiol Acetate API manufacturers, exporters, distributors and traders.

click here to find a list of Estradiol Acetate suppliers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PharmaCompass.

Estradiol Acetate NDC

National Drug Code is a comprehensive database maintained by the FDA that contains information on all drugs marketed in the US. This directory includes information about finished drug products, unfinished drug products, and compounded drug products, including those containing Estradiol Acetate as an active pharmaceutical ingredient (API).

Finished drug products

The FDA updates the NDC directory daily. The NDC numbers for Estradiol Acetate API and other APIs are published in this directory by the FDA.

Unfinished drugs

The NDC unfinished drugs database includes product listing information submitted for all unfinished drugs, such as active pharmaceutical ingredients (APIs), drugs intended for further processing and bulk drug substances for compounding.

Pharmaceutical companies that manufacture Estradiol Acetate as an active pharmaceutical ingredient (API) must furnish the FDA with an updated record of all drugs that they produce, prepare, propagate, compound, or process for commercial distribution in the US at their facilities.

Compounded drug products

The NDC directory also contains data on finished compounded human drug products that contain Estradiol Acetate and are produced by outsourcing facilities. While these outsourcing facilities are not mandated to assign a Estradiol Acetate NDC to their finished compounded human drug products, they may choose to do so.

click here to find a list of Estradiol Acetate suppliers with NDC on PharmaCompass.

Estradiol Acetate GMP

Estradiol Acetate Active pharmaceutical ingredient (API) is produced in GMP-certified manufacturing facility.

GMP stands for Good Manufacturing Practices, which is a system used in the pharmaceutical industry to make sure that goods are regularly produced and monitored in accordance with quality standards. The FDA’s current Good Manufacturing Practices requirements are referred to as cGMP or current GMP which indicates that the company follows the most recent GMP specifications. The World Health Organization (WHO) has its own set of GMP guidelines, called the WHO GMP. Different countries can also set their own guidelines for GMP like China (Chinese GMP) or the EU (EU GMP).

PharmaCompass offers a list of Estradiol Acetate GMP manufacturers, exporters & distributors, which can be sorted by USDMF, JDMF, KDMF, CEP (COS), WC, API price, and more, enabling you to easily find the right Estradiol Acetate GMP manufacturer or Estradiol Acetate GMP API supplier for your needs.

Estradiol Acetate CoA

A Estradiol Acetate CoA (Certificate of Analysis) is a formal document that attests to Estradiol Acetate's compliance with Estradiol Acetate specifications and serves as a tool for batch-level quality control.

Estradiol Acetate CoA mostly includes findings from lab analyses of a specific batch. For each Estradiol Acetate CoA document that a company creates, the USFDA specifies specific requirements, such as supplier information, material identification, transportation data, evidence of conformity and signature data.

Estradiol Acetate may be tested according to a variety of international standards, such as European Pharmacopoeia (Estradiol Acetate EP), Estradiol Acetate JP (Japanese Pharmacopeia) and the US Pharmacopoeia (Estradiol Acetate USP).

Inform the supplier about your product requirements, specifying if you need a product with particular monograph like EP (Ph. Eur.), USP, JP, BP, or any other quality. In addition, clarify whether you need hydrochloride (HCl), anhydricum, base, micronisatum or a specific level of purity. To find reputable suppliers, utilize the filters and select those certified by GMP, FDA, or any other certification as per your requirement.
For your convenience, we have listed synonyms and CAS numbers to help you find the best supplier. The use of synonyms and CAS numbers can be helpful in identifying potential suppliers, but it is crucial to note that they might not always indicate the exact same product. It is important to confirm the product details with the supplier before making a purchase to ensure that it meets your requirements.
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