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A cell-permeable, orally bioavailable, non-toxic, alkyne derivative that acts as a highly potent, and selective agonist of free fatty acid receptor 1 (FFA1; GPR40; EC50 = 20 nM in FFA1-transfected HEK-293 cells). Exhibits lower lipophilicity and excellent metabolic stability. Demonstrates over 100-fold greater selectivity over GPR43, GPR41, GPR120, PPARγ and 55 other receptors, transporters, and enzymes. Improves glucose tolerance in type 2 diabetic mice (~50 mg/kg) with efficacy comparable to DPPIV inhibitor, sitagliptin (~10 mg/kg). Displays favorable pharmacokinetic properties with t 1/2= 17 min and Cmax of 5071 (ng/ml).
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number
508941
Brand Family
Calbiochem®
Synonyms
FFA1 Agonist III, Free Fatty Acid Receptor 1 Agonist III
References
References
Christiansen, E., et al. 2013. J. Med. Chem.56, 982.
Christiansen, E., et al. 2013. J. Med. Chem.56, 982.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
07-March-2014 JSW
Synonyms
FFA1 Agonist III, Free Fatty Acid Receptor 1 Agonist III
Description
A cell-permeable, orally bioavailable, non-toxic, alkyne derivative that acts as a highly potent, and selective agonist of free fatty acid receptor 1 (FFA1; GPR40; EC50 = 20 nM in FFA1-transfected HEK-293 cells). Exhibits lower lipophilicity and excellent metabolic stability. Demonstrates over 100-fold greater selectivity over GPR43, GPR41, GPR120, PPARγ and 55 other receptors, transporters, and enzymes. Improves glucose tolerance in type 2 diabetic mice (~50 mg/kg) with efficacy comparable to DPPIV inhibitor, sitagliptin (~10 mg/kg). Displays favorable pharmacokinetic properties with t 1/2= 17 min and Cmax of 5071 (ng/ml).
Form
Off-white powder
Intert gas (Yes/No)
Packaged under inert gas
CAS number
1206628-99-0
Chemical formula
C₁₉H₁₅NO₂
Structure formula
Purity
≥98% by HPLC
Solubility
DMSO (100 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Christiansen, E., et al. 2013. J. Med. Chem.56, 982.
