V1a/V2 antagonist 1
V1a/V2 antagonist 1 (Compound 18j) is an orally active dual V1a and V2 receptor antagonist with high binding affinity for both receptors (Ki: 0.13 nM for hV1a, 0.53 nM for hV2 and 0.5 nM for mV1a; IC50: 2.2 nM for hV1a). V1a/V2 antagonist 1 inhibits Oxytocin (HY-17571)-induced scratching behavior in mice.
For research use only. We do not sell to patients.
- Formula: C25H26ClN5O3
- Molecular Weight:479.96
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Vasopressin Receptor Isoforms
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Biological Activity
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human V1a Receptor 0.13 nM (Ki) |
human V2 Receptor 0.53 nM (Ki) |
human V1a Receptor 2.2 nM (IC50) |
V1a/V2 antagonist 1 (1 μM) exhibits good hepatic microsomal metabolic stability, with Clint (h/r/m) (μL/min/mg) of 15.9/36.9/ 27.1[1].
V1a/V2 antagonist 1 has no interaction with hERG (IC50: >30 μM), and shows PDR value of 0.91 (VB-Caco-2 permeability assay)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:OT-induced scratching in mice [1]
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Dosage:0.1, 0.3, 1, 3 mg/kg
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Administration:Oral gavage (p.o.), 60-min pretreatment
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Result:Inhibited scratching with inhibition rate of 86% (3 mg/kg), 91% (1 mg/kg), 85% (0.3 mg/kg) and 81% (0.1 mg/kg).
Chemical Information
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Molecular Weight 479.96
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Formula C25H26ClN5O3
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SMILES
ClC1=CC=C2N3C(N(CC4)CCN4C5=C(OCC6)C6=CC=C5)=NN=C3CC7(OCCO7)CC2=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
V1a/V2 antagonist 1 Related Classifications
HY-168742 Related Classifications
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