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GPR81 agonist 1

Name: GPR81 agonist 1
Brand: TargetMol
SKU: T62656
Price: 132 USD
Availability: InStock
Rating: 5 (10 reviews)

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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

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Purity: 99.68%

Catalog No. T62656Cas No. 1620992-67-7

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$132	In Stock	In 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]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.68%

Appearance:Solid

Color:White

Resource Download

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 Weight	446.63
Formula	C₂₂H₃₀N₄O₂S₂
Cas No.	1620992-67-7
Smiles	C[C@H]1CC[C@@H](CC1)C(=O)Nc1nc(c(CC(=O)N2CCN(C)CC2)s1)-c1cccs1

Storage & Solubility Information

Storage

Powder: -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

	1mg	5mg	10mg	50mg
1 mM	2.2390 mL	11.1949 mL	22.3899 mL	111.9495 mL
5 mM	0.4478 mL	2.2390 mL	4.4780 mL	22.3899 mL
10 mM	0.2239 mL	1.1195 mL	2.2390 mL	11.1949 mL
20 mM	0.1119 mL	0.5597 mL	1.1195 mL	5.5975 mL
50 mM	0.0448 mL	0.2239 mL	0.4478 mL	2.2390 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 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, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

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 TargetMol | reagent 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 TargetMol | reagent 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 TargetMol | reagent 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.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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