Sitagliptin phosphate

• CAT Number: I004469
• CAS Number: 654671-78-0
• Molecular Formula: C16H15F6N5O • H3PO4
• Molecular Weight: 505.31
• Purity: ≥95%
• Synonyms: (3R)-3-amino-1-[5,6-dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)-1-butanone, monophosphate
• Target: DPP-4
• Solubility: 10 mM in DMSO, 10 mM in H2O
• Storage: Store at -20°C
• IUPAC Name: (3R)-3-amino-1-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;phosphoric acid
• InChI: InChI=1S/C16H15F6N5O.H3O4P/c17-10-6-12(19)11(18)4-8(10)3-9(23)5-14(28)26-1-2-27-13(7-26)24-25-15(27)16(20,21)22;1-5(2,3)4/h4,6,9H,1-3,5,7,23H2;(H3,1,2,3,4)/t9-;/m1./s1
• InChIKey: IQFYVLUXQXSJJN-SBSPUUFOSA-N
• SMILES: C1CN2C(=NN=C2C(F)(F)F)CN1C(=O)C[C@@H](CC3=CC(=C(C=C3F)F)F)N.OP(=O)(O)O

Sitagliptin phosphate（Cat No.:I004469）is an oral antidiabetic medication and selective dipeptidyl peptidase-4 (DPP-4) inhibitor, used to manage blood glucose levels in type 2 diabetes. By inhibiting DPP-4, sitagliptin increases the activity of incretin hormones, which stimulate insulin release and reduce glucagon levels, particularly after meals, helping to improve glycemic control. It is often used in combination with other antidiabetic agents and has a favorable safety profile, with a low risk of hypoglycemia. Sitagliptin phosphate offers an effective option for long-term diabetes management, improving blood glucose stability and patient outcomes.

Reference

[1]. Thomas, L., et al., (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylm ethyl)-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. 325(1): p. 175-82.

[2]. 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.

[3]. Sangle, G.V., et al., Novel biological action of the dipeptidylpeptidase-IV inhibitor, sitagliptin, as a glucagon-like peptide-1 secretagogue. Endocrinology, 2012. 153(2): p. 564-73.

[4]. 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.

[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.