司帕生坦
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
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。
Sparsentan (PS-433540, RE-021, DARA) 是endothelin type A receptor(ETA)和angiotensin II type 1 receptor的双重拮抗剂。 | 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.
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 |
|---|---|---|---|---|---|
| 2026-03-03 | S6665 | 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 | 2mg | 3270.55 |
| 2025-12-22 | 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 | 254740-64-2 | 5mg | 642 |
