1. GPCR/G Protein
    Membrane Transporter/Ion Channel
  2. GPR40
    Potassium Channel
  3. GW9508

GW9508 

Cat. No.: HY-15589 Purity: 99.19%
Handling Instructions

GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities.

For research use only. We do not sell to patients.

GW9508 Chemical Structure

GW9508 Chemical Structure

CAS No. : 885101-89-3

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10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
10 mg USD 50 In-stock
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50 mg USD 160 In-stock
Estimated Time of Arrival: December 31
100 mg USD 290 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities[1][2][3][4].

IC50 & Target

pEC50: 7.32 (GPR40) and 5.46 (GPR120)[1]

In Vitro

GW9508 stimulates intracellular Ca2+ mobilization in HEK-293 cells expressing GPR40 (pEC50 of 7.32) or GPR120 (pEC50 of 5.46), but not in the parent HEK-293 cell line[1].
GW9508 produces a concentration-dependent increase (pEC50 of 6.14) in glucose-stimulated insulin secretion at high glucose levels (25 mM). This resulted in a 1.52-fold increase in insulin secretion with 20 μM GW9508 in the presence of 25 mM glucose, compared with 25 mM glucose alone. The ability of GW9508 (10 μM) to enhance insulin secretion from MIN6 cells is significantly enhanced as glucose concentrations are increased[1].
GW9508 inhibits CCL17 and CCL5 expression in a pertussis toxin-sensitive manner. The inhibitory effect by GW9508 is abrogated by depletion of GPR40 with RNA interference. GW9508 further suppresses expression of IL-11, IL-24, and IL-33 induced in HaCaT cells by TNF-α and IFN-γ. GW9508 also inhibits CCL5 and CXCL10 production by normal human epidermal keratinocytes[2].

In Vivo

Administration of GW9508 200 (μM) topically to the skin suppresses ear swelling in a repeated hapten application model (BALB/c and C57BL/6 mice) and contact hypersensitivity with downregulation of CCL5 and CXCL10, respectively[2].

Molecular Weight

347.41

Formula

C₂₂H₂₁NO₃

CAS No.

885101-89-3

SMILES

O=C(O)CCC1=CC=C(NCC2=CC=CC(OC3=CC=CC=C3)=C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (287.84 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8784 mL 14.3922 mL 28.7844 mL
5 mM 0.5757 mL 2.8784 mL 5.7569 mL
10 mM 0.2878 mL 1.4392 mL 2.8784 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.20 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.20 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.20 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

GW9508GW 9508GW-9508GPR40Potassium ChannelFree fatty acid receptor 1FFAR1FFA1G-protein-coupled receptor 40KcsAGPR120glucose-sensitiveinsulinKATPTNF-αIFN-γCCL5CXCL10anti-inflammatoryanti-atheroscleroticInhibitorinhibitorinhibit

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GW9508
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