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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/<a href="/target/GPR" style="display: inline; color: #c13a36">GPR</a>40, EC50: 6 nM for hFFA1).

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TUG-770, CAS 1402601-82-4

Pack Size	Availability	Price/USD	Quantity
50 mg	Inquiry	$ 1,000.00
100 mg	Inquiry	$ 1,669.00

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Purity: 98%

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	hFFA1:6 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 2 years

Solubility Information

H2O: Insoluble

DMSO: 100 mg/mL (325.39 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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

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