Sitagliptin (phosphate) [CAS 654671-78-0]

Sitagliptin (MK-0431) phosphate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes[1][2][3][4][5].

[654671-78-0]

C16H18F6N5O5P

505.31

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

Dipeptidyl Peptidase; Endogenous Metabolite; ERK; GLP Receptor; PKA

DPP-4

99.64

DMSO : 100 mg/mL (ultrasonic) |H2O : 50 mg/mL (ultrasonic)

4°C (Powder, sealed storage, away from moisture and light)

Room Temperature

H302, H315, H319, H335

H302, H315, H319, H335