Sparsentan

Sparsentan is a dual antagonist of angiotensin II type 1 (AT1) and endothelin receptor type A (ETA, Kis = 0.8 and 9.3 nM, respectively, for the human receptors). It is selective for these receptors over AT2 and ETB receptors (Kis = >10 µM for both). Sparsentan inhibits angiotensin II-induced pressor responses in conscious normotensive rats (ED50 = 3.6 µmol/kg, p.o). It reduces mean arterial pressure in spontaneously hypertensive rats when administered orally at doses of 10, 30, or 100 µmol/kg per day. Dietary administration of sparsentan (1,800 ppm) reduces albuminuria and inhibits development of glomerulosclerosis in the gddY mouse model of IgA nephropathy.Formal Name: 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. CAS Number: 254740-64-2. Molecular Formula: C32H40N4O5S. Formula Weight: 592.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: Soluble. SMILES: CCCCC(N(CC1=CC=C(C2=C(S(NC3=NOC(C)=C3C)(=O)=O)C=CC=C2)C(COCC)=C1)C4=O)=NC54CCCC5. InChi Code: InChI=1S/C32H40N4O5S/c1-5-7-14-29-33-32(17-10-11-18-32)31(37)36(29)20-24-15-16-26(25(19-24)21-40-6-2)27-12-8-9-13-28(27)42(38,39)35-30-22(3)23(4)41-34-30/h8-9,12-13,15-16,19H,5-7,10-11,14,17-18,20-21H2,1-4H3,(H,34,35). InChi Key: WRFHGDPIDHPWIQ-UHFFFAOYSA-N.