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Conivaptan hydrochloride

Catalog No. T6453 CAS 168626-94-6

Synonyms: Vaprisol, Conivaptan HCl, YM 087

Conivaptan hydrochloride (Vaprisol) is an orally active vasopressin V2 and V1A receptor antagonist, used in the therapy of hypervolemic hyponatremia and euvolemic.

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Conivaptan hydrochloride Chemical Structure

Conivaptan hydrochloride, CAS 168626-94-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 37.00
10 mg	In stock	$ 59.00
25 mg	In stock	$ 132.00
50 mg	In stock	$ 238.00
100 mg	In stock	$ 397.00
200 mg	In stock	$ 597.00
1 mL * 10 mM (in DMSO)	In stock	$ 65.00

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Purity: 100%

Purity: 99.86%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Conivaptan hydrochloride (Vaprisol) is an orally active vasopressin V2 and V1A receptor antagonist, used in the therapy of hypervolemic hyponatremia and euvolemic.
Targets&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.

Synonyms	Vaprisol, Conivaptan HCl, YM 087
Molecular Weight	535.04
Formula	C32H26N4O2·HCl
CAS No.	168626-94-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 7 mg/mL (13.08 mM)

DMSO: 99 mg/mL (185 mM)

References and Literature

1. Wada K, et al. Eur J Pharmacol,2005, 507(1-3), 145-151. 2. Fernández-Varo G, et al. J Hepatol. 2003 Jun;38(6):755-61. 3. Yatsu T, et al. Eur J Pharmacol,1999, 376(3), 239-246.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Membrane Protein-targeted Compound Library Anti-Cancer Approved Drug Library Inhibitor Library GPCR Compound Library Drug Repurposing Compound Library CNS-Penetrant Compound Library NO PAINS Compound Library Bioactive Compounds Library Max

Related Products

Related compounds with same targets

Invopressin [Deamino-Pen1,Val4,D-Arg8]-vasopressin Vasopressin Dimer (anti-parallel) (TFA) LIXIVAPTAN Atosiban Desmopressin acetate (16679-58-6 free base) Argipressin Nelivaptan

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Keywords

Conivaptan hydrochloride 168626-94-6 GPCR/G Protein Vasopressin Receptor inhibit Vaprisol YM087 Conivaptan Conivaptan HCl Conivaptan Hydrochloride YM-087 Inhibitor YM 087 inhibitor

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