TUG-770FFA1/GPR40 agonist CAS# 1402601-82-4 |
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Quality Control & MSDS
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| Cas No. | 1402601-82-4 | SDF | Download SDF |
| PubChem ID | 66553168 | Appearance | Powder |
| Formula | C19H14FNO2 | M.Wt | 307.32 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 100 mg/mL (325.39 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 3-[4-[2-[2-(cyanomethyl)phenyl]ethynyl]-2-fluorophenyl]propanoic acid | ||
| SMILES | C1=CC=C(C(=C1)CC#N)C#CC2=CC(=C(C=C2)CCC(=O)O)F | ||
| Standard InChIKey | KIZUBVPJNPVIIN-UHFFFAOYSA-N | ||
| Standard 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) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| 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: GPR40
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 (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: References: | |||||
TUG-770 Dilution Calculator
TUG-770 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.2539 mL | 16.2697 mL | 32.5394 mL | 65.0787 mL | 81.3484 mL |
| 5 mM | 0.6508 mL | 3.2539 mL | 6.5079 mL | 13.0157 mL | 16.2697 mL |
| 10 mM | 0.3254 mL | 1.627 mL | 3.2539 mL | 6.5079 mL | 8.1348 mL |
| 50 mM | 0.0651 mL | 0.3254 mL | 0.6508 mL | 1.3016 mL | 1.627 mL |
| 100 mM | 0.0325 mL | 0.1627 mL | 0.3254 mL | 0.6508 mL | 0.8135 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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IC50: 6 nM
TUG-770 is a potent free fatty acid receptor 1 (FFA1/GPR40) agonist. Free fatty acid receptor 1 (FFA1 or GPR40) enhances the glucose-stimulated insulin secretion from pancreatic β-cells and attracts high interest as a new target for the treatment of type 2 diabetes.
In vitro: TUG-770 showed a pronounced increase in potency on FFA1 with EC50 = 6 nM and 150-fold selectivity over FFA4. TUG-770 showed a high selectivity over FFA2, FFA3, PPARγ, and 54 diverse transporters, receptors, and enzymes. In the rat INS-1E cell line, TUG-770 caused significantly increased insulin secretion at high glucose concentration and, as expected, no effect at low glucose concentration [1].
In vivo: Pharmacokinetic studies of TUG-770 in mice showed a fast oral absorption, higher plasma concentration, a longer half-life, lower clearance, and increased bioavailability. No adverse effects were seen in mice after four weeks of daily oral treatment of 20 mg/kg and acute treatment in doses up to 250 mg/kg. In vivo examination of TUG-770 in an acute intraperitoneal glucose tolerance test in normal mice showed a good dose-dependent response with maximal reduction in glucose level reached at 50 mg/kg. The followed chronic oral glucose tolerance test study in DIO mice showed that TUG-770 was more effective than its analog. Further evaluation of TUG-770 in rats confirmed a significant glucose lowering effect for the high doses [1].
Clinical trial: N/A
Reference:
[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.
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Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes.[Pubmed:23687558]
ACS Med Chem Lett. 2013 May 9;4(5):441-445.
Free fatty acid receptor 1 (FFA1 or GPR40) enhances glucose-stimulated insulin secretion from pancreatic beta-cells and currently attracts high interest as a new target for the treatment of type 2 diabetes. We here report the discovery of a highly potent FFA1 agonist with favorable physicochemical and pharmacokinetic properties. The compound efficiently normalizes glucose tolerance in diet-induced obese mice, an effect that is fully sustained after 29 days of chronic dosing.
