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GW9508 GPR agonist

Name: GW9508
Brand: Selleck Chemicals
SKU: S8014
Rating: 5 (12 reviews)

Cat.No.S8014

GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, and stimulates insulin secretion in a glucose-sensitive manner.

Chemical Structure

Molecular Weight: 347.41

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Quality Control

Batch: S801401 DMSO]69 mg/mL]false]Ethanol]69 mg/mL]false]Water]Insoluble]false Purity: 99.73%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.73

Related Targets	Adrenergic Receptor Estrogen/progestogen Receptor Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR
Other GPR Inhibitors	ONC212 Fasiglifam(TAK-875) Hemihydrate AH7614 3-chloro-5-hydroxybenzoic Acid JMS-17-2 GSK1292263 AZD1981 TC-G-1008 (GPR39-C3) SNAP94847 hydrochloride 6-OAU

Chemical Information, Storage & Stability

Molecular Weight	347.41	Formula	C₂₂H₂₁NO₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	885101-89-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC=C(C=C1)OC2=CC=CC(=C2)CNC3=CC=C(C=C3)CCC(=O)O

Solubility

In vitro
Batch:

DMSO : 69 mg/mL (198.61 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 69 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 40%PEG300 2 2%Tween80 3 56%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.000mg/ml (5.76mM)	Taking the 1 mL working solution as an example, add 20 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 560 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	The effects of GW9508 on insulin secretion are reversed by GW1100, while linoleic acid-stimulated insulin secretion is partially attenuated by GW1100.
Targets/IC₅₀/Ki	GPR40 7.32(pEC50) GPR120 5.46(pEC50)
In vitro	GW9508 is shown to be at least 100-fold selective against 220 other GPCRs, 60 kinases, 63 proteases, seven integrins and 20 nuclear receptors including PPARα, δ and γ (pEC50 4.0, 4 and 4.9, respectively). This compound produces a concentration-dependent increase in intracellular Ca²⁺ concentrations via GPR40 receptor activation and the GPR120 receptor. It is active as an agonist at both GPR40 and GPR120, it is approximately 100-fold selective for GPR40 with respect to GPR120. This chemical produces a concentration-dependent increase (pEC50=6.14) in glucose-stimulated insulin secretion at high glucose levels (25 mM). It dose dependently stimulated insulin secretion in a glucose-sensitive manner in MIN6 cells. Furthermore, this compound is able to potentiate the KCl-mediated increase in insulin secretion in MIN6 cells. It induced hyperpolarization and opening of K_ATP channels in rat β-cells. This chemical inhibits CCL17 and CCL5 expression in a pertussis toxin-sensitive manner. It further suppresses expression of IL-11, IL-24, and IL-33 induced in HaCaT cells by TNF-α and IFN-γ. It also inhibits CCL5 and CXCL10 production by normal human epidermal keratinocytes.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16702987/ [2] https://pubmed.ncbi.nlm.nih.gov/18550787/ [3] https://pubmed.ncbi.nlm.nih.gov/21593768/

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