Clazosentan

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Clazosentan

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

180384-56-9

Ro 61-1790
VML 588
AXV-034343

Clazosentan (Ro 61-1790) 是一种选择性的内皮素 A 受体 (ET_Areceptor) 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 selectiveendothelin A (ET_A) receptorantagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction^[1]^[5].

体外研究
(In Vitro)

Clazosentan (0.1 μM) inhibits the ET_Areceptor in cerebral arteries^[3].
Clazosentan is a substrate of the organic anion-transporting polypeptide (OATP) 1B1/1B3^[5].

体内研究
(In Vivo)

Clazosentan (10 μM, 0.05 mL/kg, intracisternal injection) inhibits the contractile responses to ET-1 in rats^[2].
Clazosentan (10 mg/kg, s.c.) inhibits IL-33-induced hypernociception in mice^[4].

Animal Model:	Rats^[2]
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.

Clinical Trial

分子量

577.57

性状

Solid

Formula

C₂₅H₂₃N₉O₆S

CAS 号

180384-56-9

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

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。