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Chemistry

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Also known as: 1616372-41-8, Amezalpat [inn], 1eq4lqn9n3, Orb2945076, Schembl15832811, Bdbm617517
Molecular Formula
C34H41N3O4
Molecular Weight
555.7  g/mol
InChI Key
KUPVZYDOHAPPNF-UHFFFAOYSA-N
FDA UNII
1EQ4LQN9N3

Amezalpat
Amezalpat is an orally bioavailable, small molecule, selective and competitive antagonist of peroxisome proliferator activated receptor alpha (PPARa), with potential immunomodulating and antineoplastic activities. Upon oral administration, amezalpat targets, binds to and blocks the activity of PPARa, thereby blocking transcription of PPARa target genes leading to an intracellular metabolism shift from fatty acid oxidation (FAO) to glycolysis in FAO-dependent tumors and reducing the production of fatty acids in the tumor microenvironment (TME). As fatty acids are essential for tumor cell growth in FAO-dependent tumor cells and are needed for the metabolism of suppressive immune cells in the TME, including regulatory T-cells (Tregs), reducing the amount of fatty acids leads to a direct killing of FAO-dependent tumor cells. It also skews macrophages from the immune suppressive M2 phenotype to an effector M1 phenotype and facilitates the cytotoxicity of immune effector cells, thereby stimulating an anti-tumor immune response and further killing tumor cells. Amezalpat also restores the natural inhibitor of angiogenesis thrombospondin-1 (TSP-1) and stimulator of interferon genes (STING) in the TME. PPARa, a ligand-activated nuclear transcription factor and metabolic checkpoint, regulates the expression of FAO genes and lipid metabolism. It plays a key role in immunosuppression in the TME. FAO is a metabolic pathway essential to tumor growth, survival and immunosuppression.
1 2D Structure

Amezalpat

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
2-[5-[3-[3-[1-[(4-tert-butylphenyl)methyl]-4-ethyl-5-oxo-1,2,4-triazol-3-yl]propyl]phenyl]-2-ethoxyphenyl]acetic acid
2.1.2 InChI
InChI=1S/C34H41N3O4/c1-6-36-31(35-37(33(36)40)23-25-14-17-29(18-15-25)34(3,4)5)13-9-11-24-10-8-12-26(20-24)27-16-19-30(41-7-2)28(21-27)22-32(38)39/h8,10,12,14-21H,6-7,9,11,13,22-23H2,1-5H3,(H,38,39)
2.1.3 InChI Key
KUPVZYDOHAPPNF-UHFFFAOYSA-N
2.2 Other Identifiers
2.2.1 UNII
1EQ4LQN9N3
2.3 Synonyms
2.3.1 Depositor-Supplied Synonyms

1. 1616372-41-8

2. Amezalpat [inn]

3. 1eq4lqn9n3

4. Orb2945076

5. Schembl15832811

6. Bdbm617517

7. Us20240041837, Example 6

8. Us20240041837, Example 11

9. [1,1'-biphenyl]-3-acetic Acid, 3'-[3-[1-[[4-(1,1-dimethylethyl)phenyl]methyl]-4-ethyl-4,5-dihydro-5-oxo-1h-1,2,4-triazol-3-yl]propyl]-4-ethoxy-

10. 3'-(3-(1-((4-(1,1-dimethylethyl)phenyl)methyl)-4-ethyl-4,5-dihydro-5-oxo-1h-1,2,4-triazol-3-yl)propyl)-4-ethoxy(1,1'-biphenyl)-3-acetic Acid

2.4 Create Date
2014-07-28
3 Chemical and Physical Properties
Molecular Weight 555.7 g/mol
Molecular Formula C34H41N3O4
XLogP36.8
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count5
Rotatable Bond Count13
Exact Mass Da
Monoisotopic Mass Da
Topological Polar Surface Area82.4
Heavy Atom Count41
Formal Charge0
Complexity891
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1

ABOUT THIS PAGE

Looking for 1616372-41-8 / Amezalpat API manufacturers, exporters & distributors?

Amezalpat manufacturers, exporters & distributors 1

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

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

API | Excipient name

Amezalpat

Synonyms

1616372-41-8, Amezalpat [inn], 1eq4lqn9n3, Orb2945076, Schembl15832811, Bdbm617517

Cas Number

1616372-41-8

Unique Ingredient Identifier (UNII)

1EQ4LQN9N3

About Amezalpat

Amezalpat is an orally bioavailable, small molecule, selective and competitive antagonist of peroxisome proliferator activated receptor alpha (PPARa), with potential immunomodulating and antineoplastic activities. Upon oral administration, amezalpat targets, binds to and blocks the activity of PPARa, thereby blocking transcription of PPARa target genes leading to an intracellular metabolism shift from fatty acid oxidation (FAO) to glycolysis in FAO-dependent tumors and reducing the production of fatty acids in the tumor microenvironment (TME). As fatty acids are essential for tumor cell growth in FAO-dependent tumor cells and are needed for the metabolism of suppressive immune cells in the TME, including regulatory T-cells (Tregs), reducing the amount of fatty acids leads to a direct killing of FAO-dependent tumor cells. It also skews macrophages from the immune suppressive M2 phenotype to an effector M1 phenotype and facilitates the cytotoxicity of immune effector cells, thereby stimulating an anti-tumor immune response and further killing tumor cells. Amezalpat also restores the natural inhibitor of angiogenesis thrombospondin-1 (TSP-1) and stimulator of interferon genes (STING) in the TME. PPARa, a ligand-activated nuclear transcription factor and metabolic checkpoint, regulates the expression of FAO genes and lipid metabolism. It plays a key role in immunosuppression in the TME. FAO is a metabolic pathway essential to tumor growth, survival and immunosuppression.

Amezalpat Manufacturers

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

Amezalpat Suppliers

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

Amezalpat GMP

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

Amezalpat CoA

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

Amezalpat CoA mostly includes findings from lab analyses of a specific batch. For each Amezalpat 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.

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