Bioactivity | TC-G 1005 is a potent, selective and orally active agonist of the BA receptor Takeda G protein-coupled receptor 5 (TGR5), with EC50s of 0.72 and 6.2 nM for hTGR5 and mTGR5, respectively. TC-G 1005 can reduce glucose levels in vivo[1][2]. | ||||||||||||
Target | IC50: 0.72 nM (hTGR5); 6.2 nM (mTGR5) | ||||||||||||
Invitro | TC-G 1005 activates human and mouse TGR5 with EC50s of 0.72 nM and 6.2 nM, respectively[1]. | ||||||||||||
In Vivo | TC-G 1005 (25-100 mg/kg; a single p.o.) stimulates GLP-1 secretion in imprinting control region (ICR) mice[1].TC-G 1005 (50 mg/kg; a single p.o.) causes a 49% reduction in blood glucose AUC0-120 min in ICR mice[1].TC-G 1005 (50 mg/kg; a single p.o.) significantly reduces blood glucose at 4, 6, 10, and 24 h in db/db mice[1].TC-G 1005 (5 mg/kg; p.o.) exhibits rather low plasma exposure, with a Cmax of 56 ng/mL and a t1/2 of 1.5 in rats[1]. Animal Model: | ||||||||||||
Name | TC-G 1005 | ||||||||||||
CAS | 1415407-60-1 | ||||||||||||
Formula | C25H25N3O2 | ||||||||||||
Molar Mass | 399.48 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Duan H, et, al. Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists. J Med Chem. 2012 Dec 13;55(23):10475-89. [2]. Urso A, et, al. Bile acids inhibit cholinergic constriction in proximal and peripheral airways from humans and rodents. Am J Physiol Lung Cell Mol Physiol. 2020 Feb 1;318(2):L264-L275. |