1. GPCR/G Protein
  2. GPR40
  3. TUG-770

TUG-770 

Cat. No.: HY-15697 Purity: 99.59%
Handling Instructions

TUG-770 is a potent, selective and orally active GPR40/FFA1 agonist with an EC50 of 6 nM for human FFA1. TUG-770 shows a high selectivity for FFA1 over FFA2, FFA3, FFA4, PPARγ, other receptors, transporters, and enzymes. TUG-770 can be uesd for type 2 diabetes research.

For research use only. We do not sell to patients.

TUG-770 Chemical Structure

TUG-770 Chemical Structure

CAS No. : 1402601-82-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 306 In-stock
Estimated Time of Arrival: December 31
5 mg USD 278 In-stock
Estimated Time of Arrival: December 31
10 mg USD 426 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1008 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1680 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

TUG-770 is a potent, selective and orally active GPR40/FFA1 agonist with an EC50 of 6 nM for human FFA1. TUG-770 shows a high selectivity for FFA1 over FFA2, FFA3, FFA4, PPARγ, other receptors, transporters, and enzymes. TUG-770 can be uesd for type 2 diabetes research[1].

IC50 & Target

EC50: 6 nM (Human GPR40/FFA1)[1]

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[1].
TUG-770 exhibits lower potency on the rodent orthologs (mFFA1, pEC50 = 6.83; rFFA1, pEC50 = 6.49)[1].
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)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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) [1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C56B1/6 male mice (5-6 weeks of age) fed on the 60% fat diet D12492[1]
Dosage: 20 mg/kg
Administration: Oral administration; daily; for 28 days
Result: Significantly improved glucose tolerance.
Molecular Weight

307.32

Formula

C₁₉H₁₄FNO₂

CAS No.

1402601-82-4

SMILES

FC1=C(CCC(O)=O)C=CC(C#CC2=C(CC#N)C=CC=C2)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (325.39 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2539 mL 16.2697 mL 32.5394 mL
5 mM 0.6508 mL 3.2539 mL 6.5079 mL
10 mM 0.3254 mL 1.6270 mL 3.2539 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.13 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.13 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

TUG-770TUG770TUG 770GPR40Free fatty acid receptor 1FFAR1FFA1G-protein-coupled receptor 40β-cellsglucoseinsulindiabetesInhibitorinhibitorinhibit

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Product Name:
TUG-770
Cat. No.:
HY-15697
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