Conivaptan HCl , ≥99% , 168626-94-6

CAS NO.：168626-94-6

Empirical Formula: C32H26N4O2.HCl

Molecular Weight: 535.04

MDL number: MFCD00945712

EINECS: 1312995-182-4

PRODUCT Properties

• Melting point: >250°
• storage temp.: under inert gas (nitrogen or Argon) at 2-8°C
• solubility: DMSO (Slightly), Methanol (Slightly)
• form: Solid
• color: White to Off-White
• InChIKey: BTYHAFSDANBVMJ-UHFFFAOYSA-N
• SMILES: C12=CC=CC=C1N(CCC1N=C(C)NC2=1)C(=O)C1=CC=C(NC(=O)C2C=CC=CC=2C2=CC=CC=C2)C=C1.Cl

Description and Uses

Conivaptan is an antagonist of the arginine vasopressin (AVP) receptors V_1A and V₂ (K_is = 0.48 and 3.04 nM for rat liver V_1A and kidney V₂, respectively). It also competitively inhibits oxytocin binding to rat uterine oxytocin receptors (K_i = 44 nM) but has no effect on AVP binding to anterior pituitary V_1B receptors at concentrations up to 100 μM in a radioligand binding assay. Conivaptan suppresses AVP-induced increases in intracellular calcium in vascular smooth muscle cells (VSMCs) in vitro and the pressor response in pithed rats. Conivaptan (0.01-0.3 mg/kg, i.v.) increases urine output and decreases urine osmolality in dehydrated conscious rats in a dose-dependent manner. It also reduces brain edema and blood-brain barrier disruption in a mouse experimental stroke model.

Used in treatment of congestive heart failure.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302
• Precautionary statements: P501-P270-P264-P301+P312+P330