货号:A277387 同义名: YM 087;Conivaptan (hydrochloride)
Conivaptan HCl is an inhibitor of antidiuretic hormone or antagonist of vasopressin receptor. It can inhibit rat liver V1A receptor and kidney V2 receptor with Ki of 0.48 nM and 3.04 nM, respectively.
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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。 |
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 | Not Applicable | Withdrawn(Only 1 patient recru...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 |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
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 |
动物实验配方 |