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GW9508

Cat. No. M2020

GW9508 Structure
Size Price Availability Quantity
10mg USD 70 In stock
50mg USD 250 In stock
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Quality Control
Biological Activity

GW9508 is a selective FFA1/GPR40 agonist (pEC50 values are 7.32, < 4.3 and < 4.3 for FFA1, FFA2 and FFA3 receptors respectively). GPR40 was formerly an orphan G protein-coupled receptor whose endogenous ligands have now been identified as free fatty acids (FFAs). GW9508 showed greater than 500-fold selectivity for GPR40 over GPR41 and GPR43 and possessed a good in vitro and in vivo profile with excellent bioavailability. GW9508 inhibited CCL17 and CCL5 expression in a pertussis toxin-sensitive manner. GW9508 also inhibited CCL5 and CXCL10 production by normal human epidermal keratinocytes. Administration of GW9508 topically to the skin in the challenging phase suppressed ear swelling in a repeated hapten application model and contact hypersensitivity with downregulation of CCL5 and CXCL10, respectively. GW9508 dose dependently potentiated glucose-stimulated insulin secretion in MIN6 cells, but not in primary rat or mouse islets. Furthermore, GW9508 was able to potentiate the KCl-mediated increase in insulin secretion in MIN6 cells.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 347.41
Formula C22H21NO3
CAS Number 885101-89-3
Purity >99%
Solubility DMSO 20 mg/mL
Storage at -20°C
References

A GPR40 agonist GW9508 suppresses CCL5, CCL17, and CXCL10 induction in keratinocytes and attenuates cutaneous immune inflammation.
Fujita T, et al. J Invest Dermatol. 2011 Aug;131(8):1660-7. PMID: 21593768.

Activation of ATP-sensitive potassium channels in rat pancreatic beta-cells by linoleic acid through both intracellular metabolites and membrane receptor signalling pathway.
Zhao YF, et al. J Endocrinol. 2008 Sep;198(3):533-40. PMID: 18550787.

Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules.
Briscoe CP, et al. Br J Pharmacol. 2006 Jul;148(5):619-28. PMID: 16702987.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GW9508 supplier, GPR, inhibitors

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