TUG-770

TUG-770 is a Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes. Free fatty acid receptor 1 (FFA1 or GPR40) enhances glucose-stimulated insulin secretion from pancreatic β-cells and currently attracts high interest as a new target for the treatment of type 2 diabetes.

Product information

CAS Number: 1402601-82-4

Molecular Weight: 307.32

Formula: C19H14FNO2

Synonym:

TUG 770

Chemical Name: 3-[4-[2-[2-(cyanomethyl)phenyl]ethynyl]-2-fluorophenyl]propanoic acid

Smiles: N#CCC1=CC=CC=C1C#CC1=CC(F)=C(CCC(O)=O)C=C1

InChiKey: KIZUBVPJNPVIIN-UHFFFAOYSA-N

InChi: InChI=1S/C19H14FNO2/c20-18-13-14(6-8-17(18)9-10-19(22)23)5-7-15-3-1-2-4-16(15)11-12-21/h1-4,6,8,13H,9-11H2,(H,22,23)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

TUG-770 (Compound 22) displays excellent physicochemical and in vitro ADME properties, with good aqueous solubility, good chemical stability, low lipophilicity, and decreased plasma protein binding (PPB). TUG-770 shows excellent stability toward human liver microsomes (HLM), and good permeability in the Caco-2 cell assay. TUG-770 exhibits lower potency on the rodent orthologs (mFFA1, pEC50 = 6.83; rFFA1, pEC50 = 6.49). In the rat INS-1E cell line, TUG-770 significantly increases insulin secretion (10.75% of total content with 10 μM 22 vs 8.74 with vehicle) at high glucose concentration (12.4 mM) and, no effect (4.14% of total content with 10 μM 22 vs 4.02 with vehicle) at low glucose concentration (2.8 mM).

In Vivo:

TUG-770 (Compound 22; 20 mg/kg; oral administration; daily; for 28 days) treatment significantly improves glucose tolerance, and has no effect on food intake, body weight, body composition or plasma leptin concentration. TUG-770 also significantly improves the insulin sensitivity index (plasma glucose x plasma insulin) .

References:

1. Christiansen E, Hansen SV, Urban C, Hudson BD, Wargent ET, Grundmann M, Jenkins L, Zaibi M, Stocker CJ, Ullrich S, Kostenis E, Kassack MU, Milligan G, Cawthorne MA, Ulven T. 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. Epub 2013 Apr 8. PubMed PMID: 23687558; PubMed Central PMCID: PMC3654565.

Products are for research use only. Not for human use.