Clazosentan Ro 61-1790; VML 588; AXV-034343|cas:180384-56-9|西域试剂

Clazosentan Ro 61-1790; VML 588; AXV-034343,98.01%

产品编号：Bellancom-17352| CAS NO：180384-56-9| 分子式：C₂₅H₂₃N₉O₆S| 分子量：577.57

克拉唑森坦（Ro 61-1790）是一种选择性内皮素a（ETA）受体拮抗剂。克拉唑森坦抑制ET-1介导的血管收缩。克拉唑森坦预防脑血管痉挛，血管痉挛相关的脑梗死[5]。

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货号	价格	库存与货期
Bellancom-17352	￥2500.00	杭州北京（现货）
Bellancom-17352	￥4200.00	杭州北京（现货）
Bellancom-17352	￥9200.00	杭州北京（现货）
Bellancom-17352	￥15000.00	杭州北京（现货）

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Clazosentan Ro 61-1790; VML 588; AXV-034343

产品介绍

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^[5].

体外研究

Clazosentan (0.1 μM) inhibits the ET_A receptor in cerebral arteries.
Clazosentan is a substrate of the organic anion-transporting polypeptide (OATP) 1B1/1B3^[5].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Rats
Dosage:	10 μM, 0.05 mL/kg
Administration:	Intracisternal injection
Result:	Inhibited the contractile responses to ET-1, without preventing SAH-induced upregulation of ET receptors in cerebral arteries.

体内研究

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^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Rats
Dosage:	10 μM, 0.05 mL/kg
Administration:	Intracisternal injection
Result:	Inhibited the contractile responses to ET-1, without preventing SAH-induced upregulation of ET receptors in cerebral arteries.

性状

Solid

溶解性数据

In Vitro:

DMSO : 83.33 mg/mL (144.28 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7314 mL	8.6570 mL	17.3139 mL
5 mM	0.3463 mL	1.7314 mL	3.4628 mL
10 mM	0.1731 mL	0.8657 mL	1.7314 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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
	-20°C	1 month

参考文献

. 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. [Content Brief]

. 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. [Content Brief]

. Vatter H, et al. Cerebrovascular characterization of clazosentan, the first nonpeptide endothelin receptor antagonist clinically effective for the treatment of cerebral vasospasm. Part I: inhibitory effect on endothelin(A) receptor-mediated contraction. J Neurosurg. 2005 Jun;102(6):1101-7. [Content Brief]

[4]. Verri WA Jr, Guerrero AT, Fukada SY, Valerio DA, Cunha TM, Xu D, Ferreira SH, Liew FY, Cunha FQ. IL-33 mediates antigen-induced cutaneous and articular hypernociception in mice. Proc Natl Acad Sci U S A. 2008 Feb 19;105(7):2723-8. [Content Brief]

[5]. Juif PE, et al. Influence of Rifampin-Mediated Organic Anion-Transporting Polypeptide 1B1/1B3 Inhibition on the Pharmacokinetics of Clazosentan. Clin Transl Sci. 2019 Sep;12(5):440-444. [Content Brief]

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产品编号(Item Number)

批号(Lot Number)

Clazosentan Ro 61-1790; VML 588; AXV-034343,98.01%

Clazosentan Ro 61-1790; VML 588; AXV-034343

化学品安全说明书(MSDS)

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