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GPR81 agonist 1

🥰Excellent
Catalog No. T62656Cas No. 1620992-67-7

GPR81 agonist 1 is a potent and selective GPR81 agonist with high affinity for human and mouse GPR81, inhibiting lipolysis of differentiated 3T3-L1 adipocytes, improving insulin sensitivity and glycaemic control in mouse models of insulin resistance and diabetes, and can be used in the study of diabetes and obesity.

GPR81 agonist 1

GPR81 agonist 1

🥰Excellent
Purity: 99.68%
Catalog No. T62656Cas No. 1620992-67-7
GPR81 agonist 1 is a potent and selective GPR81 agonist with high affinity for human and mouse GPR81, inhibiting lipolysis of differentiated 3T3-L1 adipocytes, improving insulin sensitivity and glycaemic control in mouse models of insulin resistance and diabetes, and can be used in the study of diabetes and obesity.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$132In StockIn Stock
5 mg$328-In Stock
10 mg$562-In Stock
25 mg$1,050-In Stock
50 mg$1,590-In Stock
1 mL x 10 mM (in DMSO)$292-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.68%
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COA HPLC HNMR

Product Introduction

Bioactivity
Description
GPR81 agonist 1 is a potent and selective GPR81 agonist with high affinity for human and mouse GPR81, inhibiting lipolysis of differentiated 3T3-L1 adipocytes, improving insulin sensitivity and glycaemic control in mouse models of insulin resistance and diabetes, and can be used in the study of diabetes and obesity.
In vitro
GPR81 agonist 1 (1-1000 nM) inhibits fat breakdown in differentiated 3T3-L1 adipocytes[1].
In vivo
GPR81 agonist 1, when administered intraperitoneally at a dose of 100 mg/kg, inhibits fat breakdown in mice without causing skin flushing and exhibits good bioavailability[1].
Chemical Properties
Molecular Weight446.63
FormulaC22H30N4O2S2
Cas No.1620992-67-7
SmilesC[C@H]1CC[C@@H](CC1)C(=O)Nc1nc(c(CC(=O)N2CCN(C)CC2)s1)-c1cccs1
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 30 mg/mL (67.17 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.48 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2390 mL11.1949 mL22.3899 mL111.9495 mL
5 mM0.4478 mL2.2390 mL4.4780 mL22.3899 mL
10 mM0.2239 mL1.1195 mL2.2390 mL11.1949 mL
20 mM0.1119 mL0.5597 mL1.1195 mL5.5975 mL
50 mM0.0448 mL0.2239 mL0.4478 mL2.2390 mL

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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 mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (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 DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.
1 Enter information below:
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g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

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

Keywords

GPR81
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