(Rac) -Sitagliptin

(Rac) -Sitagliptin is an isoform of Sitagliptin (HY-13749), which is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts[1].

Product Specifications

CAS Number

[823817-56-7]

Product Name Alternative

(Rac) -MK-0431

UNSPSC

12352005

Hazard Statement

H315-H319-H320

Target

Autophagy; Dipeptidyl Peptidase

Type

Reference compound

Related Pathways

Autophagy; Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/rac-sitagliptin.html

Solubility

10 mM in DMSO

Smiles

O=C(N1CC2=NN=C(C(F)(F)F)N2CC1)CC(N)CC3=CC(F)=C(F)C=C3F

Molecular Formula

C16H15F6N5O

Molecular Weight

407.31

Precautions

P264-P280-P302+P352-P305+P351+P338-P362

References & Citations

[1]Beconi, M.G., et al. Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs. Drug Metab Dispos, 2007. 35 (4) : p. 525-32.|[2]Thomas, L., et al. (R) -8- (3-amino-piperidin-1-yl) -7-but-2-ynyl-3-methyl-1- (4-methyl-quinazolin-2-ylmethyl) -3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with other dipeptidyl peptidase-4 inhibitors. J Pharmacol Exp Ther. 2008 Apr;325 (1) :175-82.|[3]Kim, S.J., et al., Dipeptidyl peptidase IV inhibition with MK0431 improves islet graft survival in diabetic NOD mice partially via T-cell modulation. Diabetes, 2009. 58 (3) : p. 641-51.|[4]Sangle, G.V., et al., Novel biological action of the dipeptidylpeptidase-IV inhibitor, sitagliptin, as a GLP-1 secretagogue. Endocrinology, 2012. 153 (2) : p. 564-73.|[5]Kim, S.J., et al., Inhibition of dipeptidyl peptidase IV with sitagliptin (MK0431) prolongs islet graft survival in streptozotocin-induced diabetic mice. Diabetes, 2008. 57 (5) : p. 1331-9.