SR49059 is a potent and selective non-peptide vasopressin V1A receptor antagonist which is devoid of agonist activity. SR49059 displays high affinity and efficacy at both rat (Ki = 1.6 nM) and human (Ki = 1.1 - 6.3 nM) V1A receptors and potently antagonizes arginine vasopressin-induced effects in vitro (IC50 = 3.7 nM for inhibition of human platelet aggregation) and is orally active in vivo.
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产品名称 | Vasopressin receptor 1 ↓ ↑ | Vasopressin receptor 2 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
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Conivaptan hydrochloride | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | SR 49059 is a potent, orally active, and selective antagonist of the vasopressin V1a receptor, with a Ki value of 1.4 nM[1]. |
体内研究 | Demonstrating neuroprotective properties, SR 49059 administered intraperitoneally at doses of 2 mg/kg and 30 mg/kg provides protection in models of ischemic brain injury, particularly when given shortly after occlusion of the middle cerebral artery (MCA)[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.61mL 0.32mL 0.16mL |
8.06mL 1.61mL 0.81mL |
16.12mL 3.22mL 1.61mL |
CAS号 | 150375-75-0 |
分子式 | C28H27Cl2N3O7S |
分子量 | 620.501 |
别名 | Relcovaptan |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 105 mg/mL(169.22 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |