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Chemistry

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Also known as: Sitaxsentan, 184036-34-8, Tbc-11251, N-(4-chloro-3-methyl-1,2-oxazol-5-yl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]thiophene-3-sulfonamide, Tbc11251, Ipi-1040
Molecular Formula
C18H15ClN2O6S2
Molecular Weight
454.9  g/mol
InChI Key
PHWXUGHIIBDVKD-UHFFFAOYSA-N
FDA UNII
J9QH779MEM

Sitaxentan
Sitaxentan was marketed under the trade name Thelin for the treatment of pulmonary arterial hypertension (PAH) by Encysive Pharmaceuticals until Pfizer purchased Encysive in February 2008. In 2010, Pfizer voluntarily removed sitaxentan from the market over concerns of hepatotoxicity.
1 2D Structure

Sitaxentan

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
N-(4-chloro-3-methyl-1,2-oxazol-5-yl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]thiophene-3-sulfonamide
2.1.2 InChI
InChI=1S/C18H15ClN2O6S2/c1-9-5-13-14(26-8-25-13)7-11(9)6-12(22)17-15(3-4-28-17)29(23,24)21-18-16(19)10(2)20-27-18/h3-5,7,21H,6,8H2,1-2H3
2.1.3 InChI Key
PHWXUGHIIBDVKD-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CC1=CC2=C(C=C1CC(=O)C3=C(C=CS3)S(=O)(=O)NC4=C(C(=NO4)C)Cl)OCO2
2.2 Other Identifiers
2.2.1 UNII
J9QH779MEM
2.3 Synonyms
2.3.1 MeSH Synonyms

1. N-(4-chloro-3-methyl-5-isoxazolyl)-2-((4,5-(methylenedioxy)-o-toly)acetyl)-3-thiophenesulfonamide

2. N-(4-chloro-3-methyl-5-isoxazolyl)-2-(3,4-(methylenedioxy)-6-methyl)phenylacetyl-3-thiophenesulfonamide

3. Sitaxsentan

4. Tbc 11251

5. Tbc-11251

6. Tbc11251

2.3.2 Depositor-Supplied Synonyms

1. Sitaxsentan

2. 184036-34-8

3. Tbc-11251

4. N-(4-chloro-3-methyl-1,2-oxazol-5-yl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]thiophene-3-sulfonamide

5. Tbc11251

6. Ipi-1040

7. J9qh779mem

8. Chembl282724

9. N-(4-chloro-3-methyl-5-isoxazolyl)-2-((4,5-(methylenedioxy)-o-toly)acetyl)-3-thiophenesulfonamide

10. N-(4-chloro-3-methyl-5-isoxazolyl)-2-(3,4-(methylenedioxy)-6-methyl)phenylacetyl-3-thiophenesulfonamide

11. Tbc 11251

12. Sitaxentan [inn]

13. Ipi 1040

14. Sitaxentan [usan:inn]

15. Unii-j9qh779mem

16. Sitaxsentan [mi]

17. Sitaxentan (usan/inn)

18. Sitaxentan [usan]

19. Dsstox_cid_31462

20. Dsstox_rid_97348

21. Sitaxentan [who-dd]

22. Dsstox_gsid_57673

23. 3-thiophenesulfonamide, N-(4-chloro-3-methyl-5-isoxazolyl)-2-((6-methyl-1,3-benzodioxol-5-yl)acetyl)-

24. N-(4-chloro-3-methyl-5-isoxazolyl)-2-((2-methyl-4,5-methylenedioxyphenyl)acetyl)thiophene-3-sulfonamide

25. N-(4-chloro-3-methyl-5-isoxazolyl)-2-((3,4-(methylenedioxy)-6-methylphenyl)acetyl)-3-thiophenesulfonamide

26. Schembl803344

27. Gtpl3950

28. Dtxsid0057673

29. Chebi:135736

30. Bcp13848

31. Zinc1481831

32. Tox21_113725

33. Bdbm50058126

34. Zinc328577260

35. Cs-0402

36. Db06268

37. Sb19551

38. Ncgc00253587-01

39. Hy-76520

40. N-(4-chloro-3-methylisoxazol-5-yl)-2-(2-(6-methylbenzo-[d][1,3]dioxol-5-yl)acetyl)thiophene-3-sulfonamide

41. Db-065456

42. Tbc11251 / Tbc-11251

43. Cas-184036-34-8

44. Ft-0701871

45. D07171

46. A927076

47. Q905664

48. Sr-01000945028

49. Sr-01000945028-1

50. 2-[2-(6-methyl-benzo[1,3]dioxol-5-yl)-acetyl]-thiophene-3-sulfonic Acid (4-chloro-3-methyl-isoxazol-5-yl) Amide

51. 2-[2-(6-methyl-benzo[1,3]dioxol-5-yl)-acetyl]-thiophene-3-sulfonic Acid (4-chloro-3-methyl-isoxazol-5-yl)-amide

52. 2-[2-(6-methyl-benzo[1,3]dioxol-5-yl)-acetyl]-thiophene-3-sulfonic Acid (4-chloro-3-methyl-isoxazol-5-yl)-amide (sitaxsentan)

53. N- (4- Chloro- 3- Methyl- Oxazol- 5- Yl)- 2- [2- (6- Methylbenzo[1,3]dioxol- 5- Yl)acetyl]- Thiophene- 3- Sulfonamide

54. N-(4-chloro-3-methyl-1,2-oxazol-5-yl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]thiophene-3-sulfonamide.

55. N-(4-chloro-3-methyl-1,2-oxazol-5-yl)-2-[2-(6-methyl-2h-1,3-benzodioxol-5-yl)acetyl]thiophene-3-sulfonamide

56. N-(4-chloro-3-methyl-5-isoxazolyl)-2-[(6-methyl-1,3-benzodioxol-5-yl) Acetyl]-3-thiophenesulphonamide

57. N-(4-chloro-3-methyloxazol-5-yl)-2-[2-(6-methylbenzo[1,3]dioxol-5-yl)acetyl]thiophene-3-sulfonamide

2.4 Create Date
2005-08-09
3 Chemical and Physical Properties
Molecular Weight 454.9 g/mol
Molecular Formula C18H15ClN2O6S2
XLogP33.7
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count9
Rotatable Bond Count6
Exact Mass454.0060062 g/mol
Monoisotopic Mass454.0060062 g/mol
Topological Polar Surface Area144 Ų
Heavy Atom Count29
Formal Charge0
Complexity720
Isotope Atom Count0
Defined Atom Stereocenter Count0
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

Investigated for use/treatment in pulmonary hypertension, connective tissue diseases, hypertension, and congestive heart failure.


5 Pharmacology and Biochemistry
5.1 Pharmacology

Sitaxentan belongs to a class of drugs known as endothelin receptor antagonists (ERAs). Patients with PAH have elevated levels of endothelin, a potent blood vessel constrictor, in their plasma and lung tissue. Sitaxentan blocks the binding of endothelin to its receptors, thereby negating endothelin's deleterious effects.


5.2 MeSH Pharmacological Classification

Endothelin Receptor Antagonists

Compounds and drugs that bind to and inhibit or block the activation of ENDOTHELIN RECECPTORS. (See all compounds classified as Endothelin Receptor Antagonists.)


5.3 ATC Code

C - Cardiovascular system

C02 - Antihypertensives

C02K - Other antihypertensives

C02KX - Antihypertensives for pulmonary arterial hypertension

C02KX03 - Sitaxentan


5.4 Absorption, Distribution and Excretion

Absorption

70-100%


Route of Elimination

Renal (50 to 60%) Fecal (40 to 50%)


5.5 Metabolism/Metabolites

Hepatic (CYP2C9- and CYP3A4-mediated)


5.6 Biological Half-Life

10 hours


5.7 Mechanism of Action

Sitaxentan is a competitive antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors. Under normal conditions, endothelin-1 binding of ET-A or ET-B receptors causes pulmonary vasoconstriction. By blocking this interaction, Sitaxentan decreases pulmonary vascular resistance. Sitaxentan has a higher affinity for ET-A than ET-B.


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Sitaxentan manufacturers, exporters & distributors 1

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

API | Excipient name

Sitaxentan

Synonyms

Sitaxsentan, 184036-34-8, Tbc-11251, N-(4-chloro-3-methyl-1,2-oxazol-5-yl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]thiophene-3-sulfonamide, Tbc11251, Ipi-1040

Cas Number

210421-64-0

Unique Ingredient Identifier (UNII)

J9QH779MEM

About Sitaxentan

Sitaxentan was marketed under the trade name Thelin for the treatment of pulmonary arterial hypertension (PAH) by Encysive Pharmaceuticals until Pfizer purchased Encysive in February 2008. In 2010, Pfizer voluntarily removed sitaxentan from the market over concerns of hepatotoxicity.

Sitaxentan Manufacturers

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

Sitaxentan Suppliers

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

Sitaxentan GMP

Sitaxentan 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 Sitaxentan 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 Sitaxentan GMP manufacturer or Sitaxentan GMP API supplier for your needs.

Sitaxentan CoA

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

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

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