254740-64-2
254740-64-2 结构式
基本信息
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
RE-021
PS433540
Sparsentan
BMS-346567
Sparsentan (RE-021)
Sparsentan(PS433540)
formerly known as DARA
Sparsentan-d5 (RE-021-d5)
PS433540
RE-021
FORMERLY KNOWN AS DARA
物理化学性质
常见问题列表
司帕生坦通过同时阻断内皮素A型（ETA）受体和血管紧张素II 1型（AT1）受体，抑制两者介导的肾脏炎症与纤维化信号通路，从而减缓疾病进展。作为首个非免疫抑制治疗的IgA肾病靶向药物，司帕生坦突破了传统支持疗法（如降压、降蛋白尿）及免疫抑制治疗的局限，获FDA授予突破性疗法和孤儿药资格。其加速批准基于Ⅲ期临床试验中期分析显示的蛋白尿显著减少（疾病进展关键风险指标），为IgA肾病患者提供了首个针对疾病核心机制的创新疗法。
| Target | Value |
|
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.
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2025/05/22 | 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 Sparsentan | 254740-64-2 | 5mg | 642元 |
| 2025/05/22 | 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 Sparsentan | 254740-64-2 | 10mM * 1mLin DMSO | 837元 |
| 2025/05/22 | 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 Sparsentan | 254740-64-2 | 10mg | 1044元 |