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V1a/V2 antagonist 1
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Catalog No. T203525
V1a/V2 antagonist 1 (Compound 18j) is an orally active dual-target antagonist of V1a and V2 receptors, exhibiting high binding affinity toward these receptors [Ki values are hV1a: 0.13 nM, hV2: 0.53 nM, and mV1a: 0.5 nM; IC50 for hV1a is 2.2 nM]. This compound can inhibit oxytocin-induced scratching behavior in mice.
V1a/V2 antagonist 1
V1a/V2 antagonist 1
😃Good
Catalog No. T203525
V1a/V2 antagonist 1 (Compound 18j) is an orally active dual-target antagonist of V1a and V2 receptors, exhibiting high binding affinity toward these receptors [Ki values are hV1a: 0.13 nM, hV2: 0.53 nM, and mV1a: 0.5 nM; IC50 for hV1a is 2.2 nM]. This compound can inhibit oxytocin-induced scratching behavior in mice.
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Product Introduction
Bioactivity
Chemical Properties
| Description | V1a/V2 antagonist 1 (Compound 18j) is an orally active dual-target antagonist of V1a and V2 receptors, exhibiting high binding affinity toward these receptors [Ki values are hV1a: 0.13 nM, hV2: 0.53 nM, and mV1a: 0.5 nM; IC50 for hV1a is 2.2 nM]. This compound can inhibit oxytocin-induced scratching behavior in mice. |
| Targets&IC50 | V2 receptor (human):0.53 nM (Ki), V1a receptor (human):2.2 nM, V1a receptor (human):0.13 nM (Ki) |
| In vitro | V1a/V2 antagonist 1 (1 μM) demonstrates excellent liver microsomal metabolic stability with Cl int (h/r/m) (μL/min/mg) values of 15.9/36.9/27.1. It exhibits no interaction with hERG (IC 50: >30 μM), and has a PDR value of 0.91 according to the VB-Caco-2 permeability assay. |
| In vivo | A V1a/V2 antagonist 1, administered orally at doses of 0.1-3 mg/kg with a 60-minute pretreatment, significantly inhibits Oxytocin-induced scratching behavior in mice. |
| Molecular Weight | 479.96 |
| Formula | C25H26ClN5O3 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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