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GW9508

Cat. No. M2020
GW9508 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 55  USD55 In stock
10mg USD 50  USD50 In stock
50mg USD 160  USD160 In stock
100mg USD 275  USD275 In stock
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Quality Control & Documentation
Biological Activity

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 has anti-inflammatory and anti-atherosclerotic activities. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. GW9508 has anti-inflammatory and anti-atherosclerotic activities.

Customer Product Validations & Biological Datas
Source Exp Cell Res (2013). Figure 1. GW9508
Method XTT analyzes
Cell Lines MC3T3-E1 cell
Concentrations 1 10 50 100 μM
Incubation Time 24 h
Results To determine whether cell growth inhibition was related to cytostatic effects or cell death, OcP were labeled for apoptosis and necrosis pathways as determined by annexin V/7-AAD apoptosis detection kit. According to fluorescent activating cell sorting data, when incubated with 100 mM of GW9508, cells were found positive for both markers
Chemical Information
Molecular Weight 347.41
Formula C22H21NO3
CAS Number 885101-89-3
Solubility (25°C) DMSO ≥ 80 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Fujita T, et al. J Invest Dermatol. A GPR40 agonist GW9508 suppresses CCL5, CCL17, and CXCL10 induction in keratinocytes and attenuates cutaneous immune inflammation.

[2] Zhao YF, et al. J Endocrinol. Activation of ATP-sensitive potassium channels in rat pancreatic beta-cells by linoleic acid through both intracellular metabolites and membrane receptor signalling pathway.

[3] Briscoe CP, et al. Br J Pharmacol. Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules.

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