290815-26-8

Basic information

• Product Name: avosentan
• Synonyms: avosentan;N-[6-Methoxy-5-(2-methoxyphenoxy)-2-(4-pyridinyl)-4-pyrimidinyl]-5-methyl-2-pyridinesulfonamide;Ro 67-0565;SPP-301;Avosentan (SPP301);N-(6-Methoxy-5-(2-methoxyphenoxy)-2-(pyridin-4-yl)-pyrimidin-4-yl)-5-methylpyridine-2-sulfonamide;N-(6-Methoxy-5-(2-methoxyphenoxy)-2-(pyridin-4-yl)-pyrimidin-4-yl)-5-methylpyridine-2-sulfonam;2-Pyridinesulfonamide,N-[6-methoxy-5-(2-methoxyphenoxy)-2-(4-pyridinyl)-4-pyrimidinyl]-5-methyl-
• CAS NO: 290815-26-8
• Molecular Formula: C₂₃H₂₁N₅O₅S
• Molecular Weight: 479.50834
• Mol File: 290815-26-8.mol
• Article Data: 2

Chemical Properties

• Boiling Point: 575.472 °C at 760 mmHg
• Flash Point: 301.835 °C
• Appearance: /
• Density: 1.363
• PKA: 3.19±0.10(Predicted)
• CAS DataBase Reference: avosentan(CAS DataBase Reference)
• NIST Chemistry Reference: avosentan(290815-26-8)
• EPA Substance Registry System: avosentan(290815-26-8)

Safety Data

• Hazardous Substances Data: 290815-26-8(Hazardous Substances Data)

Usage

Uses

Avosentan is a competitive antagonist of Endothelin-1 (ET-1) with a high selectivity for the ETA receptor. Avosentan may be a potential option in the treatment of glaucoma.

Enzyme inhibitor

This potent, selective and orally available endothelin A receptor blocker (FW = 479.51 g/mol; CAS 290815-26-8; Soluble in DMSO), also known by its code names SPP301 and Ro 67-0565, induces the dose-dependent reduction in the fractional renal excretion of sodium (up to 8.7% at 50 mg avosentan), with a paralleled dose-related increase in proximal sodium reabsorption. Avosentan reduces albuminuria, when added to standard treatment in patients with type 2 diabetes and overt nephropathy, but induces significant fluid overload and congestive heart failure.

Upstream product

• 290815-30-4 5-methyl-pyridine-2-sulfonic acid [6-chloro-5-(2-methoxy-phenoxy)-2-pyridin-4-yl-pyrimidin-4-yl]-amide 

Relevant articles and documents

Crystalline forms of a pyridinyl-sulfonamide and their use as endothelin receptor antagonists

Crystalline forms A and B of 5-methyl-pyridine-2-sulfonic acid [6-methoxy-5-(2-methoxy-phenoxy)-2-pyridin-4-yl-pyrimidin-4-yl]-amide of formula (1) are described, whereby form B is the most stable form. 5-methyl-pyridine-2-sulfonic acid [6-methoxy-5-(2-me