Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Conivaptan hydrochloride (Vaprisol) is an orally active vasopressin V2 and V1A receptor antagonist, used in the therapy of hypervolemic hyponatremia and euvolemic.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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5 mg | 在庫あり | ¥ 8,500 | |||
10 mg | 在庫あり | ¥ 13,500 | |||
25 mg | 在庫あり | ¥ 30,500 | |||
50 mg | 在庫あり | ¥ 55,000 | |||
100 mg | 在庫あり | ¥ 91,500 | |||
200 mg | 在庫あり | ¥ 137,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 15,000 |
説明 | Conivaptan hydrochloride (Vaprisol) is an orally active vasopressin V2 and V1A receptor antagonist, used in the therapy of hypervolemic hyponatremia and euvolemic. |
ターゲット&IC50 | V1a (rat liver):0.48nM(Ki), V2 (rat kidney):3.04 nM(Ki) |
In vivo | Conivaptan administered intravenously at doses of 0.03, 0.1, and 0.3 mg/kg increases urine volume and decreases urine osmolality in a dose-dependent manner in both myocardial infarction and sham-operated rats. In myocardial infarction rats, a dose of 0.3 mg/kg notably lowers right ventricular systolic pressure, left ventricular end-diastolic pressure, reduces lung/body weight ratio, and right atrial pressure, while significantly enhancing dP/dt(max)/left ventricular pressure. Additionally, conivaptan acutely augments urine volume, reduces osmolality, and at study conclusion, cirrhotic rats treated with the V(1a)/V(2)-AVP receptor antagonist exhibit neither hyponatremia nor hypoosmolality. It also normalizes sodium urine volume without impacting creatinine clearance or arterial pressure. At dosages ranging from 0.01 to 0.1 mg/kg i.v., conivaptan demonstrates a dose-dependent diuretic effect in dogs, effectively inhibits vasopressin-induced pressor effects, and at 0.1 mg/kg, substantially blocks vasoconstriction from exogenous vasopressin. Furthermore, at 0.1 mg/kg i.v., it significantly enhances cardiac function in dogs with congestive heart failure as demonstrated by increases in left ventricular dP/dtmax, cardiac output, and stroke volume, alongside significant reductions in left ventricular end-diastolic pressure and total peripheral vascular resistance. |
別名 | Vaprisol, Conivaptan HCl, YM 087 |
分子量 | 535.04 |
分子式 | C32H26N4O2·HCl |
CAS No. | 168626-94-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 7 mg/mL (13.08 mM)
DMSO: 99 mg/mL (185 mM)
You can also refer to dose conversion for different animals. 詳細
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Conivaptan hydrochloride 168626-94-6 GPCR/G Protein Vasopressin Receptor inhibit Vaprisol YM087 Conivaptan Conivaptan HCl Conivaptan Hydrochloride YM-087 Inhibitor YM 087 inhibitor