TUG-770

Modify Date: 2024-01-02 19:38:06

TUG-770 Structure
TUG-770 structure
Common Name TUG-770
CAS Number 1402601-82-4 Molecular Weight 307.318
Density 1.3±0.1 g/cm3 Boiling Point 523.5±50.0 °C at 760 mmHg
Molecular Formula C19H14FNO2 Melting Point N/A
MSDS N/A Flash Point 270.4±30.1 °C

 Use of TUG-770


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) [1]Target: GPR40in 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 [1].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 [1].Clinical trial:

 Names

Name 3-[4-[2-[2-(cyanomethyl)phenyl]ethynyl]-2-fluorophenyl]propanoic acid
Synonym More Synonyms

 TUG-770 Biological Activity

Description 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) [1]Target: GPR40in 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 [1].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 [1].Clinical trial:
Related Catalog
References

[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.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 523.5±50.0 °C at 760 mmHg
Molecular Formula C19H14FNO2
Molecular Weight 307.318
Flash Point 270.4±30.1 °C
Exact Mass 307.100861
PSA 61.09000
LogP 3.68
Vapour Pressure 0.0±1.4 mmHg at 25°C
Index of Refraction 1.614
Storage condition -20℃

 Synonyms

Benzenepropanoic acid, 4-[2-[2-(cyanomethyl)phenyl]ethynyl]-2-fluoro-
3-(4-((2-(cyanomethyl)phenyl)ethynyl)-2-fluorophenyl)propanoic acid
TUG-770
3-(4-{[2-(Cyanomethyl)phenyl]ethynyl}-2-fluorophenyl)propanoic acid
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Price: $306/10mM*1mLinDMSO

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