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Products are for research use only. Not for human use. We do not sell to patients.
(TUG770; TUG 770)
TUG-770 Chemical Structure
|Product name: TUG-770|
|Cat. No.: HY-15697|
TUG-770 is a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist with EC50 of 6 nM for hFFA1.
IC50 Value: 6 nM (hFFA1, EC50) 
in vitro: TUG-770 (Compound 22) displayed excellent physicochemical and in vitro ADME properties, with good aqueous solubility, good chemical stability, low lipophilicity, and decreased plasma protein binding (PPB). TUG-770 furthermore showed excellent stability toward human liver microsomes (HLM), no inhibition of selected CYP-enzymes implicated in drug-drug interactions, no P-glycoprotein (P-gp) inhibition, and good permeability in the Caco-2 cell assay .
in vivo: Examination of TUG-770 in an acute intraperitoneal glucose tolerance test (IPGTT) in normal mice revealed a good dose dependent response with maximal reduction in glucose level reached at 50 mg/kg. The effect of TUG-770 was fully sustained after 29 days of daily oral treatment. Additional evaluation of TUG-770 in rats confirmed a significant glucose lowering effect for the high doses already after 10 min and for all doses after 30 min .
|M.Wt||307.32||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||3.2539 mL||16.2697 mL||32.5394 mL|
|5 mM||0.6508 mL||3.2539 mL||6.5079 mL|
|10 mM||0.3254 mL||1.6270 mL||3.2539 mL|
GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes.
GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1.
GW 1100 is a selective antagonist of GPR40-mediated Ca2(addition) elevations in HEK293 cells stimulated by GW 9508 (an agonist of both GPR40 and GPR120, another GPCR activated by long chain fatty acids) or linoleic acid with a pIC50 value equal to 5.99.
GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner.
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