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TUG-770

Catalog No. TQ0241   CAS 1402601-82-4

TUG-770 is a highly potent agonist of free fatty acid receptor 1 (FFA1/GPR40, EC50: 6 nM for hFFA1).

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TUG-770 Chemical Structure
TUG-770, CAS 1402601-82-4
Pack Size Availability Price/USD Quantity
2 mg 5 days $ 134.00
5 mg 5 days $ 229.00
10 mg 5 days $ 352.00
1 mL * 10 mM (in DMSO) 5 days $ 252.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description TUG-770 is a highly potent agonist of free fatty acid receptor 1 (FFA1/GPR40, EC50: 6 nM for hFFA1).
Targets&IC50 FFA1/GPR40 (human):6 nM (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, no inhibition of selected CYP-enzymes implicated in drug-drug interactions, no P-glycoprotein 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.
Molecular Weight 307.32
Formula C19H14FNO2
CAS No. 1402601-82-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

DMSO: 100 mg/mL (325.39 mM)

TargetMolReferences and Literature

1. Christiansen E, Hansen SV, Urban C, Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes. ACS Med Chem Lett. 2013 May 9;4(5):441-445. 2. Urano Y, et al. Comparative hepatic transcriptome analyses revealed possible pathogenic mechanisms of fasiglifam (TAK-875)-induced acute liver injury in mice. Chem Biol Interact. 2018 Sep 20;296:185-197.

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Keywords

TUG-770 1402601-82-4 Endocrinology/Hormones GPCR/G Protein GPR TUG 770 TUG770 inhibitor inhibit

 

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