| Bioactivity | TUG-469 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes[1][2]. | ||||||||||||
| Invitro | TUG-469 (0-10 μM) shows efficacy to hFFA1 with a pEC50 value of 7.73[1].TUG-469 (10 μM) increases the insulin secretion under 10 mM glucose stimulation[1].TUG-469 (0-100 μM) is >200-fold selective for FFA1 over FFA4 with EC50 values of 19 nM and 4.4 μM for FFA1 and FFA4, respectively[2].TUG-469 (5 μM; 30 min) significantly increases insulin secretion of INS-1 cells with the presence of high glucose concentration (16.7 mM)[2]. | ||||||||||||
| In Vivo | TUG-469 (5 mg/kg; i.p.; 60 and 90 min after glucose administration) affects blood glucose level[2]. Animal Model: | ||||||||||||
| Name | TUG-469 | ||||||||||||
| CAS | 1236109-67-3 | ||||||||||||
| Formula | C23H23NO2 | ||||||||||||
| Molar Mass | 345.43 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Christiansen E, et al. Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. ACS Med Chem Lett. 2010 Jul 2;1(7):345-9. [2]. Urban C, et al. In vitro and mouse in vivo characterization of the potent free fatty acid 1 receptor agonist TUG-469. Naunyn Schmiedebergs Arch Pharmacol. 2013 Dec;386(12):1021-30. |