Sparsentan (RE-021) 是高度选择的血管紧张素 II (angiotensin II) 和内皮素 A (endothelin A) 受体的双重拮抗剂，K_i 值分别为 0.8 和 9.3 nM。

Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with K i s of 0.8 and 9.3 nM, respectively.

Solid

Ki: 0.8 nM (Human angiotensin II), 9.3 nM (Human endothelin A), 0.4 nM (Rat angiotensin II)

Sparsentan dose dependently antagonizes the angiotensin II-induced pressor response with an ED 50 value of 0.8 μmol/kg iv and 3.6 μmol/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 μmol/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 μmol/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 μmol/kg/day essentially converts the spontaneously hypertensive rats into normotensive rats during the course of its pharmacokinetic duration. has not independently confir

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Murugesan N, et al. Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. J Med Chem. 2005 Jan 13;48(1):171-9.

In Vitro: DMSO : 100 mg/mL (168.71 mM; Need ultrasonic)配制储备液