TC-G 1005_product_DataBase

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

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

PeptideDB

TC-G 1005

CAS: 1415407-60-1 F: C25H25N3O2 W: 399.48