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.
Chemical Formula: C19H14FNO2
Exact Mass: 307.1009
Molecular Weight: 307.3244
Elemental Analysis: C, 74.26; H, 4.59; F, 6.18; N, 4.56; O, 10.41
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.03.00
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).
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) .
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.
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