Clazosentan|180384-56-9|(Ro 61-1790; VML 588; AXV-034343)-陌孚医药/Medlife

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Clazosentan (Synonyms: Ro 61-1790; VML 588; AXV-034343)

目录号: PL13972 纯度: ≥98%

CAS No. :180384-56-9

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中文名称	Clazosentan
中文别名	克拉生坦
英文名称	Clazosentan
英文别名	N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)pyridin-4-yl]pyrimidin-4-yl]-5-methyl-pyridine-2-sulfonamide;Clazosentan;N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)-4-pyridinyl]-4-pyrimidinyl]-5-methyl-2-Pyridinesulfonamide;N-[6-(2-HYDROXYETHOXY)-5-(2-METHOXYPHENOXY)-2-[2-(2H-TETRAZOL-5-YL)PYRIDIN-4-YL]PYRIMIDIN-4-YL]-5-METHYL-PYRIDINE-2-SUL...;N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)pyridin-4-yl]pyrimidin-4-yl]-5-methyl-pyridine-2-sulfonami;N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)pyridin-4-yl]pyrimidin-4-yl]-5-methylpyridine-2-sulfonamide;UNII-3DRR0X4728;VML 588;Octahydroaminoacridine succinate;N-(2-(2-(2H-tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl)-5-methylpyridine-2-sulfonamide
Cas No.	180384-56-9
分子式	C₂₅H₂₃N₉O₆S
分子量	577.57
包装储存	Powder -20°C 3 years；In solvent -80°C 6 months

产品详情

Clazosentan (Ro 61-1790) 是一种选择性的内皮素 A 受体 (ET_A receptor) 拮抗剂。Clazosentan 抑制 ET-1 介导的血管收缩。Clazosentan 可预防脑血管痉挛、血管痉挛相关性脑梗死。

生物活性

Clazosentan (Ro 61-1790) is a selective endothelin A (ET A ) receptor antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction.

性状

Solid

体外研究(In Vitro)

Clazosentan (0.1 μM) inhibits the ETA receptor in cerebral arteries.
Clazosentan is a substrate of the organic anion-transporting polypeptide (OATP) 1B1/1B3.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Clazosentan (10 μM, 0.05?mL/kg, intracisternal injection) inhibits the contractile responses to ET-1 in rats.
Clazosentan (10 mg/kg, s.c.) inhibits IL-33-induced hypernociception in mice. 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；In solvent -80°C 6 months

ClinicalTrial

参考文献

[1]. Juif PE, et al. Clinical Pharmacology of Clazosentan, a Selective Endothelin A Receptor Antagonist for the Prevention and Treatment of aSAH-Related Cerebral Vasospasm. Front Pharmacol. 2021 Feb 4;11:628956.
[2]. Povlsen GK, et al. MEK1/2 inhibitor U0126 but not endothelin receptor antagonist clazosentan reduces upregulation of cerebrovascular contractile receptors and delayed cerebral ischemia, and improves outcome after subarachnoid hemorrhage in rats. J Cereb Blood Flow Metab. 2015 Feb;35(2):329-37.

溶解度数据	In Vitro: DMSO : 83.33 mg/mL (144.28 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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