rac-Sitagliptin-d4 hydrochloride

Modify Date: 2024-01-12 18:38:42

rac-Sitagliptin-d4 hydrochloride Structure
rac-Sitagliptin-d4 hydrochloride structure
Common Name rac-Sitagliptin-d4 hydrochloride
CAS Number 1620233-77-3 Molecular Weight 411.34
Density N/A Boiling Point N/A
Molecular Formula C16H12D4ClF6N5O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of rac-Sitagliptin-d4 hydrochloride


(Rac)-Sitagliptin-d4((Rac)-MK-0431-d4) hydrochloride is a labelled racemic Sitagliptin. Sitagliptin (MK-0431) hydrochloride is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts[1].

 Names

Name rac-Sitagliptin-d4 hydrochloride

 rac-Sitagliptin-d4 hydrochloride Biological Activity

Description (Rac)-Sitagliptin-d4((Rac)-MK-0431-d4) hydrochloride is a labelled racemic Sitagliptin. Sitagliptin (MK-0431) hydrochloride is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts[1].
Related Catalog
In Vitro Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
References

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

[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.

[6]. 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.

 Chemical & Physical Properties

Molecular Formula C16H12D4ClF6N5O
Molecular Weight 411.34