Formulation: A crystalline solid
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
Purity: ≥98%
Formula Markup: C32H40N4O5S
Formula Weight: 592,7
Shelf life (days): 1460
CAS Number: 254740-64-2
Notes: 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).{60287} 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.{60288}
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