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GSK137647A

Cat. No. M5187
GSK137647A Structure
Synonym:

GSK 137647

Size Price Availability Quantity
5mg USD 50  USD50 In stock
10mg USD 80  USD80 In stock
50mg USD 260  USD260 In stock
100mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

GSK137647A is a selective FFAR4 (GRP120) agonist for human, Mouse and Rat FFA4 with pEC50 values of 6.3, 6.2 and 6.1, respectively. GSK137647A is shown to provide at least 100-fold selectivity against the panel which included 41 G-protein-coupled receptors. Under high glucose conditions (25 mM), GSK137647A produces a concentration-dependent increase in glucose stimulated insulin secretion. GSK137647A induces insulin secretion and inhibits epithelial ion transport, GSK137647A is related to regulation of glucose homeostasis and anti-inflammatory response. GSK137647A has anti-inflammatory activity.

Chemical Information
Molecular Weight 305.39
Formula C16H19NO3S
CAS Number 349085-82-1
Solubility (25°C) DMSO 90 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] Sparks SM, et al. Bioorg Med Chem Lett. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).

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  Catalog
Abmole Inhibitor Catalog




Keywords: GSK137647A, GSK 137647 supplier, GPR/FFAR, inhibitors, activators


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