A vasopressin V1A and V2 receptor antagonist
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Labeled Version(s)
26455Conivaptan-d4
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Conivaptan (hydrochloride)

Item No. 23728

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[(4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl]-[1,1'-biphenyl]-2-carboxamide, monohydrochloride
CAS Number
168626-94-6
Synonyms
  • YM-087
Molecular Formula
C32H26N4O2 • HCl
Formula Weight
535.0
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly SolubleMethanol: Slightly Soluble
SMILES
O=C(NC1=CC=C(C(N2CCC(N=C(C)N3)=C3C4=C2C=CC=C4)=O)C=C1)C(C=CC=C5)=C5C6=CC=CC=C6.Cl
InChi Code
InChI=1S/C32H26N4O2.ClH/c1-21-33-28-19-20-36(29-14-8-7-13-27(29)30(28)34-21)32(38)23-15-17-24(18-16-23)35-31(37)26-12-6-5-11-25(26)22-9-3-2-4-10-22;/h2-18H,19-20H2,1H3,(H,33,34)(H,35,37);1H
InChi Key
BTYHAFSDANBVMJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
4°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    5 mg

    $75

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    10 mg

    $134

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    25 mg

    $295

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    50 mg

    $516

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    Product Description

    Conivaptan is an antagonist of the arginine vasopressin (AVP) receptors V1A and V2 (Kis = 0.48 and 3.04 nM for rat liver V1A and kidney V2, respectively).1 It also competitively inhibits oxytocin binding to rat uterine oxytocin receptors (Ki = 44 nM) but has no effect on AVP binding to anterior pituitary V1B 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tahara, A., Tomura, Y., Wada, K.-I., et al. Pharmacological profile of YM087, a novel potent nonpeptide vasopressin V1A and V2 receptor antagonist, in vitro and in vivo. J. Pharmacol. Exp. Ther. 282(1), 301-308 (1997).

    2. Zeynalov, E., Jones, S.M., Seo, J.W., et al. Arginine-vasopressin receptor blocker conivaptan reduces brain edema and blood-brain barrier disruption after experimental stroke in mice. PLoS One 10(8), e0136121 (2015).