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Sparsentan(RE-021)

Sparsentan(RE-021) structure

CAS No:
254740-64-2
Formula:
C32H40N4O5S
Chemical Name:
Sparsentan(RE-021)
Synonyms:
4'-((2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl)-N-(4,5-dimethylisoxazol-3-yl)-2'-(ethoxymethyl)-[1,1'-biphenyl]-2-sulfonamide;Sparsentan (RE-021);Sparsentan-d5 (RE-021-d5);RE 201;[1,1'-Biphenyl]-2-sulfonamide, 4'-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-N-(4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-;Sparsentan;4'-[(2-Butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-N-(4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-[1,1'-biphenyl]-2-sulfonamide;BMS-346567
Categories:
Active Pharmaceutical Ingredients > Other Chemical Drugs

Description

Sparsentan has been used in trials studying the treatment of Focal Segmental Glomerulosclerosis. Sparsentan is the first and only dual-acting angiotensin and endothelin receptor antagonist (DARA) in development.

Sparsentan(RE-021) Basic Attributes

Molecular Weight：

592.75

Exact Mass：

592.27194156

UNII：

9242RO5URM

Characteristics

PSA：

122.48000

XLogP3：

7.06670

Density：

1.28±0.1 g/cm3

Melting Point：

148 °C(Solv: isopropanol (67-63-0); water (7732-18-5))

Boiling Point：

744.4±70.0 °C(Predicted)

PKA：

7.06±0.50

Drug Information

Drug Indication：

Treatment of focal segmental glomerulosclerosis|Treatment of primary IgA nephropathy

Mechanism of Action：

Sparsentan, which possesses two clinically validated mechanisms of action in a single molecule, works by selectively blocking the action of two potent vasoconstrictor and mitogenic agents, angiotensin II (AII) and endothelin 1 (ET1), at their respective receptors. Sparsentan is highly selective (10,000-fold) for the AII receptor sub-type 1 and the ET receptor sub-type A. As such, Sparsentan combines the properties of an angiotensin receptor blocker (ARB) and an endothelin receptor antagonist (ERA) in the same molecule.

MeSH Entry Terms：

(1,1'-biphenyl)-2-sulfonamide, 4'-((2-butyl-4-oxo-1,3-diazaspiro(4.4)non-1-en-3-yl)methyl)-N-(4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-

Sparsentan(RE-021) Use and Manufacturing

Use Classification：

Human drugs -> Rare disease (orphan)|Human Drugs -> EU pediatric investigation plans

Computed Properties

Molecular Weight:592.8
XLogP3:5
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:8
Rotatable Bond Count:12
Exact Mass:592.27194156
Monoisotopic Mass:592.27194156
Topological Polar Surface Area:123
Heavy Atom Count:42
Complexity:1060
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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