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首页 / 抑制剂/激动剂 / G蛋白偶联受体/G蛋白 / 加压素受体 / Conivaptan HCl/盐酸考尼伐坦

Conivaptan HCl/盐酸考尼伐坦 {[allProObj[0].p_purity_real_show]}

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.

Conivaptan HCl/盐酸考尼伐坦 化学结构 CAS号：168626-94-6
Conivaptan HCl/盐酸考尼伐坦 化学结构
CAS号：168626-94-6
Conivaptan HCl/盐酸考尼伐坦 3D分子结构
CAS号：168626-94-6
Conivaptan HCl/盐酸考尼伐坦 化学结构 CAS号：168626-94-6
Conivaptan HCl/盐酸考尼伐坦 3D分子结构 CAS号：168626-94-6
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Conivaptan HCl/盐酸考尼伐坦 纯度/质量文件 产品仅供科研

货号：A277387 标准纯度： {[allProObj[0].p_purity_real_show]}
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产品名称 Vasopressin receptor 1 ↓ Vasopressin receptor 2 ↓ 其他靶点 纯度
Conivaptan HCl ✔ 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。

Conivaptan HCl/盐酸考尼伐坦 生物活性

靶点

  • Vasopressin receptor 1
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].

Conivaptan HCl/盐酸考尼伐坦 临床研究

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 - -

Conivaptan HCl/盐酸考尼伐坦 参考文献

[1]Wada K, Fujimori A, et al. Intravenous administration of conivaptan hydrochloride improves cardiac hemodynamics in rats with myocardial infarction-induced congestive heart failure. Eur J Pharmacol. 2005 Jan 10;507(1-3):145-51.

[2]Fernandez-Varo G, Ros J, et al. Effect of the V1a/V2-AVP receptor antagonist, Conivaptan, on renal water metabolism and systemic hemodynamics in rats with cirrhosis and ascites. J Hepatol. 2003 Jun;38(6):755-61.

[3]Wada K, Fujimori A, Matsukawa U, Arai Y, Sudoh K, Yatsu T, Sasamata M, Miyata K. Intravenous administration of conivaptan hydrochloride improves cardiac hemodynamics in rats with myocardial infarction-induced congestive heart failure. Eur J Pharmacol. 2005 Jan 10;507(1-3):145-51

[4]Fernández-Varo G, Ros J, Cejudo-Martín P, Cano C, Arroyo V, Rivera F, Rodés J, Jiménez W. Effect of the V1a/V2-AVP receptor antagonist, Conivaptan, on renal water metabolism and systemic hemodynamics in rats with cirrhosis and ascites. J Hepatol. 2003 Jun;38(6):755-61

[5]Yatsu T, Tomura Y, Tahara A, Wada K, Kusayama T, Tsukada J, Tokioka T, Uchida W, Inagaki O, Iizumi Y, Tanaka A, Honda K. Cardiovascular and renal effects of conivaptan hydrochloride (YM087), a vasopressin V1A and V2 receptor antagonist, in dogs with pacing-induced congestive heart failure. Eur J Pharmacol. 1999 Jul 9;376(3):239-46

Conivaptan HCl/盐酸考尼伐坦 实验方案

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

Conivaptan HCl/盐酸考尼伐坦 技术信息

CAS号168626-94-6
分子式C32H27ClN4O2
分子量 535.04
SMILES Code O=C(C1=CC=CC=C1C2=CC=CC=C2)NC3=CC=C(C(N4C5=CC=CC=C5C(NC(C)=N6)=C6CC4)=O)C=C3.[H]Cl
MDL No. MFCD00945712
别名 YM 087; Conivaptan (hydrochloride); Conivaptan HCl
运输蓝冰
InChI Key BTYHAFSDANBVMJ-UHFFFAOYSA-N
Pubchem ID 216322
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Sealed in dry,2-8°C
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
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
方案一
方案二

Tags: Conivaptan hydrochloride | YM 087;Conivaptan (hydrochloride);Conivaptan HCl | Vasopressin Receptor | AmBeed-信号通路专用抑制剂 | Conivaptan HCl/盐酸考尼伐坦 纯度/质量文件 | Conivaptan HCl/盐酸考尼伐坦 亚型比较 | Conivaptan HCl/盐酸考尼伐坦 生物活性 | Conivaptan HCl/盐酸考尼伐坦 临床数据 | Conivaptan HCl/盐酸考尼伐坦 参考文献 | Conivaptan HCl/盐酸考尼伐坦 实验方案 | Conivaptan HCl/盐酸考尼伐坦 技术信息

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