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LY2922470

Name: LY2922470
Brand: TargetMol
SKU: T15810
Price: 105 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T15810Cas No. 1423018-12-5

LY2922470 is a potent, selective G protein-coupled receptor 40 (GPR40) agonist, with EC50s of 7 nM for human GPR40, 1 nM for mouse GPR40 and 3 nM for rat GPR40, respectively. LY2922470 reduces glucose levels along and increases insulin and GLP-1 significantly.

LY2922470

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Purity: 97.08%

Catalog No. T15810Cas No. 1423018-12-5

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$105	-	In Stock
5 mg	$249	-	In Stock
10 mg	$373	-	In Stock
25 mg	$649	-	In Stock
50 mg	$926	-	In Stock
100 mg	$1,260	-	In Stock
200 mg	$1,690	-	In Stock
1 mL x 10 mM (in DMSO)	$261	-	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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Purity:97.08%

Color:White to Yellow

Resource Download

COA LCMS HNMR

Product Introduction

LY2922470 AI Summary

LY2922470 exhibits antidiabetic activity by reducing plasma glucose levels, demonstrated in albino Balb/c mice with an ED50 of 1.0 mg/kg and in Zucker fa/fa rats with an ED90 of 3.3 mg/kg. It acts as an agonist at GPR40 receptors, showing increased intracellular Ca2+ flux with an EC50 of 152.0 nM and an Emax of 84.0% in human assays. This compound also displays competitive displacement of [3H]-TAK-875 from GPR40 with a Ki of 27.0 nM and induces beta-arrestin recruitment with EC50 values ranging from 1.0 to 7.0 nM and Emax values up to 139.0%. Pharmacokinetic properties include high protein binding in plasma (>99.0%) and moderately high lipophilicity (logP = 5.2). It demonstrates high aqueous solubility at pH 7.4 (>100,000.0 nM) and solubility in various solutions ranging from 35.0 to 46.0 ug/mL. The metabolic stability of LY2922470 varies across species, exhibiting moderate intrinsic clearance in mouse, rat, dog, and human microsomes, with drug degradation percentages between 24.0% and 38.0%. Inhibition of human ERG is observed with an IC50 greater than 10,000.0 nM. Pharmacokinetic profiles include parameters such as Cmax, Tmax, half-lives, and volume of distribution in various species (mice, rats, dogs, and humans), with specific profiles noted in type 2 diabetic patients. LY2922470 also demonstrates dissociation constants (pKa) of 3.4 and 6.0. Overall, the compound shows promising pharmacological properties, including strong agonist activity at GPR40 receptors, effective hypoglycemic effects, and favorable pharmacokinetic and metabolic profiles, making it a potential candidate for further investigation in diabetes treatment..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	LY2922470 is a potent, selective G protein-coupled receptor 40 (GPR40) agonist, with EC50s of 7 nM for human GPR40, 1 nM for mouse GPR40 and 3 nM for rat GPR40, respectively. LY2922470 reduces glucose levels along and increases insulin and GLP-1 significantly.
Targets&IC50	FFA1/GPR40:1 nM(EC50,mouse), FFA1/GPR40:3 nM(EC50,rat), FFA1/GPR40:7 nM(EC50, human)

Chemical Properties

Molecular Weight	475.6
Formula	C₂₈H₂₉NO₄S
Cas No.	1423018-12-5
Smiles	COc1cccc2CCCN(Cc3ccc(COc4ccc(cc4)[C@H](CC(O)=O)C#CC)s3)c12
Relative Density.	1.247 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 125 mg/mL (262.83 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.41 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	2.1026 mL	10.5130 mL	21.0261 mL	105.1304 mL
5 mM	0.4205 mL	2.1026 mL	4.2052 mL	21.0261 mL
10 mM	0.2103 mL	1.0513 mL	2.1026 mL	10.5130 mL
20 mM	0.1051 mL	0.5257 mL	1.0513 mL	5.2565 mL
50 mM	0.0421 mL	0.2103 mL	0.4205 mL	2.1026 mL
100 mM	0.0210 mL	0.1051 mL	0.2103 mL	1.0513 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