货号:A277387 同义名: YM 087;Conivaptan (hydrochloride)
Conivaptan HCl 是抗利尿激素的拮抗剂或加压素受体的拮抗剂。它能抑制大鼠肝脏V1A受体和肾脏V2受体,Ki值分别为0.48 nM和3.04 nM。
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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 | ✔ | 98% | |||||||||||||||||
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。 |
靶点 |
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描述 | Conivaptan (Hydrochloride) is a non-peptide antagonist of vasopressin receptor, with Ki values of 0.48 and 3.04 nM for rat liver V1A receptor and rat kidney V2 receptor respectively. At 4 weeks after coronary occlusion, conivaptan (0.03, 0.1 and 0.3 mg/kg i.v.) dose-dependently increased urine volume and reduced urine osmolality in both myocardial infarction and sham-operated rats. Conivaptan (0.3 mg/kg i.v.) significantly reduced right ventricular systolic pressure, left ventricular end-diastolic pressure, lung/body weight and right atrial pressure in myocardial infarction rats. Moreover, conivaptan (0.3 mg/kg i.v.) significantly increased dP/dt(max)/left ventricular pressure[3]. Conivaptan produces an acute increase in urine volume (UV), a reduction in osmolality (UOsm) and, at the end of the investigation, cirrhotic rats receiving the V(1a)/V(2)-AVP receptor antagonist does not show hyponatremia or hypoosmolality. Conivaptan also normalizes U(Na)V without affecting creatinine clearance and arterial pressure[4]. Conivaptan (0.1 mg/kg, i.v.) improves cardiac function, as evidenced by significant increases in left ventricular dP/dtmax, cardiac output and stroke volume, and reduces preload and afterload, as evidenced by significant decreases in left ventricular end-diastolic pressure and total peripheral vascular resistance in dogs with congestive heart failure[5]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00811486 | Right Heart Failure ... 展开 >> Pulmonary Hypertension 收起 << | Not Applicable | Withdrawn(Only 1 patient recru... 展开 >>ited, and he withdrew) 收起 << | - | United States, Colorado ... 展开 >> University of Colorado at Denver and Health Sciences Center General Clinical Research Center Denver, Colorado, United States, 80262 收起 << |
NCT01954290 | Acute Cerebrovascular Accident... 展开 >> Cerebral Edema 收起 << | Phase 2 | Withdrawn(Investigator is leav... 展开 >>ing the institution.) 收起 << | - | - |
NCT00380575 | Hyponatremia | Phase 3 | Completed | - | - |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.87mL 0.37mL 0.19mL |
9.35mL 1.87mL 0.93mL |
18.69mL 3.74mL 1.87mL |
CAS号 | 168626-94-6 |
分子式 | C32H27ClN4O2 |
分子量 | 535.035 |
别名 | YM 087;Conivaptan (hydrochloride);Conivaptan HCl |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere,Room Temperature |
溶解方案 |
DMSO: 105 mg/mL(196.25 mM),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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |