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Sitagliptin

$60$72

Products Details

Product Description

– Sitagliptin (MK-0431) is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts[1].

Web ID

– HY-13749

Storage Temperature

– -20°C, 3 years; 4°C, 2 years (Powder)

Shipping

– Room Temperature

Applications

– Metabolism-protein/nucleotide metabolism

Molecular Formula

– C16H15F6N5O

Citations

– Biochem Pharmacol. 2023 Oct 5:115846.|Cell Death Dis. 2021 Oct 11;12(10):928.|Front Oncol. 24 September 2021.|iScience. 2023 Feb.|J Biol Chem. 2018 Dec 7;293(49):18864-18878. |J Sep Sci. 2021 Oct 28.|Korean J Physiol Pharmacol. 2021 Sep 1;25(5):425-437.|Neurol Res. 2018 Sep;40(9):736-743.|Nutr Neurosci. 2018 Apr 26:1-17.|Oxid Med Cell Longev. 2019 Nov 15;2019:6181754.|Oxid Med Cell Longev. 2022 May 17;2022:2586305.|Sci Rep. 2019 Mar 11;9(1):4074.|Biomed Pharmacother. 2023 Mar 24;162:114555.|bioRxiv. 2023 Nov 4.

References

– [1]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.|[2]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.|[3]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.|[4]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.|[5]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.

CAS Number

– 486460-32-6

Molecular Weight

– 407.31

Compound Purity

– 99.76

SMILES

– O=C(N1CC2=NN=C(C(F)(F)F)N2CC1)C[C@H](N)CC3=CC(F)=C(F)C=C3F

Clinical Information

– Launched

Research Area

– Metabolic Disease

Solubility

– DMSO : 50 mg/mL (ultrasonic)

Target

– Autophagy;Dipeptidyl Peptidase

Isoform

– DPP-4

Pathway

– Autophagy;Metabolic Enzyme/Protease

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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