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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.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction
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Chemical Properties
Storage & Solubility Information
| 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 | V1a receptor (human):2.2 nM, V2 receptor (human):0.53 nM (Ki), 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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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