TC-G 1005

• CAT Number: I011108
• CAS Number: 1415407-60-1
• Molecular Formula: C25H25N3O2
• Molecular Weight: 399.48
• Purity: ≥95%
• Synonyms: (4-cyclopropyl-2,3-dihydroquinoxalin-1-yl)-[4-(2,5-dimethylphenoxy)pyridin-3-yl]methanone
• InChI: InChI=1S/C25H25N3O2/c1-17-7-8-18(2)24(15-17)30-23-11-12-26-16-20(23)25(29)28-14-13-27(19-9-10-19)21-5-3-4-6-22(21)28/h3-8,11-12,15-16,19H,9-10,13-14H2,1-2H3
• InChIKey: JQULIQJSYPZQMA-UHFFFAOYSA-N
• SMILES: CC1=CC(=C(C=C1)C)OC2=C(C=NC=C2)C(=O)N3CCN(C4=CC=CC=C43)C5CC5

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].
TC-G 1005 activates human and mouse TGR5 with EC50s of 0.72 nM and 6.2 nM, respectively[1].
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].

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.
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[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.
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