2. GPCR/G Protein
  3. Vasopressin Receptor
  4. 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.

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V1a/V2 antagonist 1 Chemical Structure

V1a/V2 antagonist 1 Chemical Structure

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V1a/V2 antagonist 1 Related Antibodies

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Description

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[1].

IC50 & Target[1]

human V1a Receptor

0.13 nM (Ki)

human V2 Receptor

0.53 nM (Ki)

human V1a Receptor

2.2 nM (IC50)

In Vitro

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.

V1a/V2 antagonist 1 Related Antibodies
In Vivo

V1a/V2 antagonist 1 (0.1-3 mg/kg, p.o., 60-min pretreatment) notably inhibits Oxytocin (HY-17571)-induced scratching behavior in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: OT-induced scratching in mice [1]
Dosage: 0.1, 0.3, 1, 3 mg/kg
Administration: Oral gavage (p.o.), 60-min pretreatment
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).
Molecular Weight

479.96

Formula

C25H26ClN5O3
SMILES

ClC1=CC=C2N3C(N(CC4)CCN4C5=C(OCC6)C6=CC=C5)=NN=C3CC7(OCCO7)CC2=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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V1a/V2 antagonist 1 Related Classifications

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

V1a/V2 antagonist 1Vasopressin ReceptorScratchingGroomingPermeabilityMicrosomalVB-Caco-2CHO cellsInhibitorinhibitorinhibit

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