For research use only. Not for therapeutic Use.
AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 shows anti-hyperglycemic activity[1].
AR453588 (3-30 mg/kg; p.o) lowers post-prandial glucose in normal C57BL/6J mice[1].
AR453588 (3-30 mg/kg; p.o.; once-daily for 14 days) shows anti-hyperglycemic activity in a dose-ranging 14 day ob/ob mouse[1].
AR453588 (10 mg/kg; p.o.) treatment shows that the Tmax, AUCinf, Vss, Cmax and F are 1.0 mL/min/kg, 4.65 h μg /mL, 1.67 μg /mL and 60.3%, respectively[1].
AR453588 (1 mg/kg; i.v.) treatment shows that the CL, AUCinf, Vss, and t1/2 are 21.6 mL/min/kg, 0.77 h μg /mL, 0.746 L/kg and 1.28 hours, respectively[1].
| Catalog Number | I017350 |
| CAS Number | 1065609-00-8 |
| Synonyms | 1-[4-[5-[[3-(2-methylpyridin-3-yl)oxy-5-pyridin-2-ylsulfanylpyridin-2-yl]amino]-1,2,4-thiadiazol-3-yl]piperidin-1-yl]ethanone |
| Molecular Formula | C25H25N7O2S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C25H25N7O2S2/c1-16-20(6-5-11-26-16)34-21-14-19(35-22-7-3-4-10-27-22)15-28-24(21)30-25-29-23(31-36-25)18-8-12-32(13-9-18)17(2)33/h3-7,10-11,14-15,18H,8-9,12-13H2,1-2H3,(H,28,29,30,31) |
| InChIKey | WITGITFYEMHCEZ-UHFFFAOYSA-N |
| SMILES | CC1=C(C=CC=N1)OC2=C(N=CC(=C2)SC3=CC=CC=N3)NC4=NC(=NS4)C5CCN(CC5)C(=O)C |
| Reference | [1]. Hinklin RJ, et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorg Med Chem. 2020 Jan 1;28(1):115232. |
