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Sparsentan (PS-433540, RE-021, DARA) is a first-in-class, orally active, high-affinity dual antagonist of the endothelin type A receptor (ETA) and Angiotensin II type 1 (AT1) receptor, with Ki values of 9.3 and 0.8 nM, respectively. Sparsentan dose dependently antagonizes the angiotensin II-induced pressor response with an ED50 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 compound’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.
| Molecular Weight | 592.75 |
| Formula | C32H40N4O5S |
| CAS Number | 254740-64-2 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Efren Chavez, et al. Front Med (Lausanne). Novel Therapies for Alport Syndrome
| Related Endothelin Receptor Products |
|---|
| Zibotentan
Zibotentan (ZD4054) is a more selective and specific endothelin-A receptor (ETAR) antagonist with an IC50 value of 21 nM. |
| Ambrisentan
Ambrisentan is an orally active, highly selective antagonist of the endothelin-1 type A receptor. |
| Sitaxsentan sodium
Sitaxsentan (TBC-11251) is an orally active, highly selective antagonist of endothelin A receptors. |
| Macitentan
Macitentan is an orally-active, tissue-targeting dual ET receptor antagonist. |
| Bosentan Hydrate
Bosentan is an endothelin (ET) receptors antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively. |
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