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- MedChemExpress(MCE)
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- 2025年12月05日
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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
RE-021; DARA-a
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
254740-64-2
- 规格：
10 mM * 1 mL/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥837.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥642.0 |
| 规格： | 10 mg | 产品价格： | ￥1044.0 |
| 规格： | 25 mg | 产品价格： | ￥2100.0 |
| 规格： | 50 mg | 产品价格： | ￥3360.0 |
| 规格： | 100 mg | 产品价格： | ￥5364.0 |
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Sparsentan
CAS No. : 254740-64-2
MCE 国际站：Sparsentan
产品活性：Sparsentan (RE-021) 是高度选择的血管紧张素 II (angiotensin II) 和内皮素 A (endothelin A) 受体的双重拮抗剂，Ki 值分别为 0.8 和 9.3 nM。
研究领域：GPCR/G Protein
作用靶点：Angiotensin Receptor | Endothelin Receptor
In Vivo: 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 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.
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