中文名称:
4-[(2-丁基-4-氧代-1,3-二氮杂螺[4.4]壬-1-烯-3-基)甲基]-N-(4,5-二甲基-3-异恶唑基)-2-(乙氧基甲基)-[1,1-联苯]-2-磺酰胺
中文同义词:
4-[(2-丁基-4-氧代-1,3-二氮杂螺[4.4]壬-1-烯-3-基)甲基]-N-(4,5-二甲基-3-异恶唑基)-2-(乙氧基甲基)-[1,1-联苯]-2-磺酰胺;化合物SPARSENTAN
英文同义词:
4-((2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl)-N-(4,5-dimethylisoxazol-3-yl)-2-(ethoxymethyl)-[1,1-biphenyl]-2-sulfonamide;Sparsentan (RE-021);Sparsentan-d5 (RE-021-d5);RE 201;[1,1-Biphenyl]-2-sulfonamide, 4-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-N-(4,5-dimethyl-3-isoxazolyl)-2-(ethoxymethyl)-;Sparsentan;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;BMS-346567
熔点
148 °C(Solv: isopropanol (67-63-0); water (7732-18-5))
沸点
744.4±70.0 °C(Predicted)
密度
1.28±0.1 g/cm3(Predicted)
酸度系数(pKa)
7.06±0.50(Predicted)
生物活性
Sparsentan (PS-433540, RE-021, DARA) 是endothelin type A receptor(ETA)和angiotensin II type 1 receptor的双重拮抗剂。
靶点
Target Value
endothelin type A receptor
()
angiotensin II type 1 receptor
()
endothelin type A receptor
()
angiotensin II type 1 receptor
()
体内研究
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.
