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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:
Lu-135252
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
171714-84-4
- 规格:
10 mM * 1 mL/1 mg/5 mg/10 mg/50 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥1430.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥495.0 |
| 规格: | 5 mg | 产品价格: | ¥1300.0 |
| 规格: | 10 mg | 产品价格: | ¥2200.0 |
| 规格: | 50 mg | 产品价格: | ¥6500.0 |
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Darusentan
CAS No. : 171714-84-4
MCE 国际站:Darusentan
产品活性:Darusentan (Lu-135252) 是一种选择性内皮素受体 A (ET-A) 受体拮抗剂,其与 ET-A 受体的 Ki 为 1.4 nM,与 ET-B 受体的 Ki 为 184 nM,对 ETA 受体的选择性比 ETB 受体高100多倍。Darusentan 在大鼠主动脉血管平滑肌细胞 (RAVSMs) 膜中竞争结合放射性标记的内皮素,Ki 为 13 nM。
研究领域:GPCR/G Protein
作用靶点:Endothelin Receptor
In Vitro: Darusentan ((S)-Darusentan) competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki=13 nM. In isolated endothelium-denuded rat aortic rings, Darusentan inhibits endothelin-induced vascular contractility with a pA2=8.1±0.14. Darusentan ( 0.001-1μM) inhibits ET-1-induced signaling in cultured RAVSMs.
In Vivo: Darusentan (30 mg/kg per day orally for weeks 3 and 4) reverses aortic alterations produced by infusion of Norepinephrine (2.5 μg/kg per min subcutaneously for 2 and 4 weeks) in male Sprague Dawley rats.
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