Tezosentan|180384-57-0|(RO 610612)-陌孚医药/Medlife

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Tezosentan (Synonyms: RO 610612)

目录号: PL09355 纯度: ≥98%

CAS No. :180384-57-0

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PL09355-200mg	200mg	询价	询价
PL09355-500mg	500mg	询价	询价

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中文名称	Tezosentan
中文别名	替唑生坦;替唑生坦标准品
英文名称	Tezosentan
英文别名	N-(2-(2-(2H-Tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl)-5-isopropylpyridine-2-sulfonamide;Tezosentan;N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)pyridin-4-yl]pyrimidin-4-yl]-5-propan-2-ylpyridine-2-sulfonamide;TEZOSENTANE;2-Pyridinesulfonamide,N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(2-(1H-tetrazol-5-yl)-4-pyridinyl)-4-pyrimidinyl)-5-(1-methylethyl);N-(6-(2-Hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(2-(1H-tetrazol-5-yl)-4-pyridinyl)-4-pyrimidinyl)-5-(1-methylethyl)-2-pyridinesulfonamide;Tezosentan [INN];N-(2-(2-(2H-Tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl;N-(2-(2-(2H-Tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl)-5;N-[6-(2-Hydroxyethoxy)-5-(2-Methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)-4-pyridinyl]-4-pyriMidinyl]-5-(1-Methylethyl)-2-pyridinesulfonaMide
Cas No.	180384-57-0
分子式	C₂₇H₂₇N₉O₆S
分子量	605.63
包装储存	4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

产品详情

Tezosentan (RO 610612) 是内皮素 (ET) 受体的一个拮抗剂，其对 ET_A 和 ET_B 受体的 pA₂ 值分别为 9.5,7.7。

生物活性

Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA 2 s of 9.5, 7.7 for ET A and ET B receptors, respectively.

性状

Solid

IC50 & Target[1][2]

ETA ETA 9.5 (pA2)

体外研究(In Vitro)

Affinity of Tezosentan for the ET receptors is assessed in different cells and tissues. Tezosentan inhibits the specific I-labeled ET-1 binding to ETA receptors with an inhibitory potency (Ki) of 0.3 nM on CHO cells and of 18 nM on membranes of baculovirus-infected insect cells. Similarly, Tezosentan inhibits the specific binding of I-labeled ET-1, ET-3, or sarafotoxin S6c to ETB receptors with an inhibitory affinity of 10 to 21 nM. Tezosentan up to a concentration of 1 μM did not exhibit any binding inhibitory activity in 27 radioligand binding assays different from ET binding. On H1 central, 5-hydroxytryptamine2A, and vasopressin V1 receptors, Tezosentan (1 μM) induces a weak inhibition of less than 20%. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

In pithed Wistar rats, Tezosentan dose-dependently inhibits the pressor effect of big ET-1 (P<0.001 at all doses). At the lowest dose tested of 1 mg/kg, Tezosentan inhibits the pressor effect of the various doses of big ET-1 by 50 to 80%. Tezosentan has no effect by itself on blood pressure in these pithed rats. Tezosentan is very effective in a rat model of acute renal failure. ET antagonists have been shown to prevent the vasoconstriction and the renal failure that follow acute renal ischemia in rats. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

ClinicalTrial

参考文献

[1]. Clozel M, et al. Pharmacology of tezosentan, new endothelin receptor antagonist designed for parenteral use. J Pharmacol Exp Ther. 1999 Aug;290(2):840-6.

溶解度数据	In Vitro: DMSO : 50 mg/mL (82.56 mM; Need ultrasonic)配制储备液

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产品使用指南

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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