Conivaptan-d4
Conivaptan-d4 (YM 087-d4) is the deuterated-labeled Conivaptan (HY-18347). Conivaptan (YM 087 free base) is an orally active dual vasopressin V1a/V2 receptor antagonist with Ki values of 0.48 nM and 3.04 nM for vasopressin V1a receptor and V2 receptor, respectively. Conivaptan competitively and reversibly blocks vasopressin-mediated antidiuresis, vasoconstriction, and cellular hypertrophy, while inhibiting CYP3A4. Conivaptan inhibits vasopressin-induced intracellular calcium, cAMP, and mitogen-activated kinase activation in vascular smooth muscle cells and cardiomyocytes. Conivaptan induces water diuresis while improving hemodynamics in heart failure models, reducing left ventricular end-diastolic pressure, vascular resistance, and organ weight. Conivaptan is used for research on hyponatremia and congestive heart failure.
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- CAS No.: 1129433-63-1
- Formule: C32H22D4N4O2
- Masse moléculaire:502.60
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
IC50 & Target
[1]|
V1a Receptor 0.48 nM (Ki) |
V2 Receptor 3.04 nM (Ki) |
CYP3A4 |
Application
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 1129433-63-1
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Masse moléculaire 502.60
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Formule C32H22D4N4O2
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SMILES
O=C(C1=C([2H])C([2H])=C(NC(C2=C(C3=CC=CC=C3)C=CC=C2)=O)C([2H])=C1[2H])N4C5=CC=CC=C5C6=C(N=C(C)N6)CC4
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Synonyms
YM 087-d4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)