Darusentan|171714-84-4|(Lu-135252)-陌孚医药/Medlife

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Darusentan (Synonyms: Lu-135252)

目录号: PL13979 纯度: ≥98%

CAS No. :171714-84-4

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中文名称	Darusentan
中文别名	达卢生坦;达卢生坦标准品;达鲁生坦;达洛生坦
英文名称	Darusentan
英文别名	Darusentan;(2S)-2-(4,6-dimethoxypyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid;(+)-(S)-2-(4,6-dimethoxy-pyrimidin-2-yloxy)-3-methoxy-3,3-diphenyl-propionic acid;(+)-(S)-2-(4,6-dimethoxypyrimidine-2-yloxy)-3-methoxy-3,3-diphenylpropionic acid;henyl-,(S);HMR-4005;(2S)-2-(4,6-DIMETHOXYPYRIMIDIN-2-YL)OXY-3-METHOXY-3,3-DI(PHENYL)PROPANOIC ACID;darusentan, CID177236;FEJVSJIALLTFRP-LJQANCHMSA-N;(S)-2-((4,6-dimethoxypyrimidin-2-yl)oxy)-3-methoxy-3,3-diphenylpropanoic acid
Cas No.	171714-84-4
分子式	C₂₂H₂₂N₂O₆
分子量	410.42
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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 K_i 为 1.4 nM，与 ET-B 受体的 K_i 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，K_i 为 13 nM。

生物活性

Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a K i of 1.4 nM to the ET-A receptor and a K i of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a K i of 13 nM.

性状

Solid

体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Frank Enseleit, et al. Darusentan, a selective endothelin A receptor antagonist, for the oral treatment of resistant hypertension. Ther Adv Cardiovasc Dis. 2010 Aug;4(4):231-40.
[2]. Liang F, et al. Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries. Can J Physiol Pharmacol. 2010 Aug;88(8):840-9.

溶解度数据	In Vitro: DMSO : 100 mg/mL (243.65 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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