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司帕生坦

司帕生坦

中文名称:司帕生坦
英文名称:Sparsentan (RE-021)
CAS号:254740-64-2
分子式:C32H40N4O5S
分子量:592.75
EINECS号:
Mol文件:254740-64-2.mol
司帕生坦 结构式

司帕生坦 性质

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)
储存条件 Store at -20°C
溶解度 可溶于DMSO
形态 结晶固体
酸度系数(pKa) 7.06±0.50(Predicted)
颜色 白色至米白色
InChIKey WRFHGDPIDHPWIQ-UHFFFAOYSA-N
SMILES C1(C2=CC=C(CN3C(=O)C4(CCCC4)N=C3CCCC)C=C2COCC)=CC=CC=C1S(NC1C(C)=C(C)ON=1)(=O)=O

司帕生坦 用途与合成方法

Sparsentan (PS-433540, RE-021, DARA) 是endothelin type A receptor(ETA)和angiotensin II type 1 receptor的双重拮抗剂。
TargetValue
endothelin type A receptor
()
angiotensin II type 1 receptor
()

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.

司帕生坦 价格(试剂级)

更新日期 产品编号 产品名称 CAS号 包装 价格
2024-04-30 HY-17621 1 mg 600
2024-04-30 HY-17621 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 254740-64-2 5mg 1100

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