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GPR61 Inverse agonist 3
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Catalog No. T218882 Copy Product Info
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GPR61 Inverse agonist 3 is a selective compound capable of crossing the blood-brain barrier, functioning as an inverse agonist for GPR61. It demonstrates an IC50 of 4.0 nM for human receptors and 8.8 nM for mouse receptors, with a Ki of 0.34 nM in humans and 1.1 nM in mice. This compound disrupts the GPR61-Gαs protein interaction, thus eliminating the constitutive activity of GPR61. Additionally, GPR61 Inverse agonist 3 moderately inhibits the GABAA chloride ion channel and PDE3A1, with IC50 values of 4.6 μM and 8.9 μM, respectively. When co-administered with pan-CYP inhibitors, it shows no functional effect on food intake in adult mice. GPR61 Inverse agonist 3 can be utilized in research related to cachexia/sarcopenia.
GPR61 Inverse agonist 3
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
Bioactivity
Storage & Solubility Information
| Description | GPR61 Inverse agonist 3 is a selective compound capable of crossing the blood-brain barrier, functioning as an inverse agonist for GPR61. It demonstrates an IC50 of 4.0 nM for human receptors and 8.8 nM for mouse receptors, with a Ki of 0.34 nM in humans and 1.1 nM in mice. This compound disrupts the GPR61-Gαs protein interaction, thus eliminating the constitutive activity of GPR61. Additionally, GPR61 Inverse agonist 3 moderately inhibits the GABAA chloride ion channel and PDE3A1, with IC50 values of 4.6 μM and 8.9 μM, respectively. When co-administered with pan-CYP inhibitors, it shows no functional effect on food intake in adult mice. GPR61 Inverse agonist 3 can be utilized in research related to cachexia/sarcopenia. |
| 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.
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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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