Sparsentan

China [CN]

I. Basic Information

Item | Details

English Name | Sparsentan (RE-021)

Chinese Name | Sparsentan

CAS Number | 1217621-09-0

Chemical Name | Ethyl (2S)-2-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methoxy]phenyl]methylamino]-3-[[4-(2-methyl-2H-tetrazol-5-yl)phenyl]thio]propanoate

Molecular Formula | C₃₁H₃₄N₈O₃S

Molecular Weight | 614.72

Target | ETA receptor (Ki=12.8nM), AT1 receptor (Ki=0.36nM), >500 times selectivity for ETB/AT2 receptors

Developer | Travere Therapeutics (formerly Retrophin)

Market Launch Date | February 2023 (FDA)

Dosage Form and Strength | Film-coated tablets: 200mg, 400mg

II. Physicochemical Properties

Parameter | Data

Appearance | White to off-white crystalline powder

Solubility | Slightly soluble in water, readily soluble in DMSO and methanol

Dissociation Constant (pKa) | 8.2 (amino group), 4.5 (tetrazole) (predicted value)

Stability | Stable for 36 months at 25℃/60% RH, store in a sealed, cool, and dry place, avoid strong light/high temperature

Chiral Characteristics | Single S configuration, optical purity >99.5%

Partition Coefficient (logP) | 5.8 (neutral pH, predicted value)

BCS Classification | Class II (high permeability, low solubility)