Sparsentan

254740-64-2

C32H40N4O5S

10 mM in DMSO

GPCR/G Protein; GPCR/G Protein

Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with K_is of 0.8 and 9.3 nM, respectively. IC50 & Target: Ki: 0.8 nM (Human angiotensin II), 9.3 nM (Human endothelin A), 0.4 nM (Rat angiotensin II)^[1] In Vivo: Sparsentan dose dependently antagonizes the angiotensin II-induced pressor response with an ED₅₀ value of 0.8 umol/kg iv and 3.6 umol/kg po. Sparsentan also shows efficacious and long acting in the big ET-1-induced pressor model. Sparsentan causes a significant lowering of blood pressure at the lowest dose tested (10 umol/kg/day) in spontaneously hypertensive rats. Sparsentan shows good oral bioavailability in rats, dogs, and monkeys, averaging 40%, 86%, and 21% F, respectively. At 100 umol/kg/day, Sparsentan reduces the blood pressure from 170 to less than 100 mmHg during the course of the drug’s pharmacokinetic duration. Sparsentan at 100 umol/kg/day essentially converts the spontaneously hypertensive rats into normotensive rats during the course of its pharmacokinetic duration^[1].