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Sitagliptin phosphate

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Catalog No. T23358Cas No. 654671-78-0
Alias Sitagliptin (phosphate), MK-0431 phosphate, Januvia

Sitagliptin phosphate (MK-0431 phosphate) is a dipeptidyl peptidase-4 (DPP4) inhibitor.

Sitagliptin phosphate

Sitagliptin phosphate

🥰Excellent
Purity: 99.72%
Catalog No. T23358Alias Sitagliptin (phosphate), MK-0431 phosphate, JanuviaCas No. 654671-78-0
Sitagliptin phosphate (MK-0431 phosphate) is a dipeptidyl peptidase-4 (DPP4) inhibitor.
Pack SizePriceAvailabilityQuantity
50 mg$33In Stock
100 mg$47In Stock
200 mg$57In Stock
500 mg$94In Stock
1 mL x 10 mM (in DMSO)$52In Stock
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Purity:99.72%
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Product Introduction

Bioactivity
Description
Sitagliptin phosphate (MK-0431 phosphate) is a dipeptidyl peptidase-4 (DPP4) inhibitor.
Targets&IC50
DPP4:19 nM
In vitro
In vitro: Sitagliptin was a potent inhibitor for DPP-4 with an IC50 of 18 nM. Sitagliptin inhibited DPP-8 (IC50: 48 μM). Sitagliptin showed no effect on several related peptidases, including DPP-9, DPP-II, and aminopeptidase P [1].
In vivo
In free-fed Han-Wistar rats, the ED50 values ??for the inhibition of plasma DPP-4 activity by sitagliptin phosphate were calculated as 7 hours post-dose at 2.3 mg/kg and 24 hours post-dose at 30 mg/kg [1]. A mouse model of streptozotocin-induced type 1 diabetes showed elevated plasma DPP-4 levels, which was significantly suppressed in mice on a sitagliptin phosphate diet. This is achieved through a positive effect on hyperglycemia regulation, possibly by prolonging islet graft survival. The plasma clearance and volume of distribution of sitagliptin phosphate in rats (40-48 mL/min/kg, 7-9 L/kg) were higher than those in dogs (9 mL/min/kg, 3 L/kg); its The half-life is shorter in rats, 2 hours in dogs and 4 hours in dogs[2].
AliasSitagliptin (phosphate), MK-0431 phosphate, Januvia
Chemical Properties
Molecular Weight505.31
FormulaC16H18F6N5O5P
Cas No.654671-78-0
SmilesN[C@@H](CC(N1Cc2nnc(C(F)(F)F)n2CC1)=O)Cc(c(F)c1)cc(F)c1F.OP(O)(O)=O
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (98.95 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9790 mL9.8949 mL19.7898 mL98.9492 mL
5 mM0.3958 mL1.9790 mL3.9580 mL19.7898 mL
10 mM0.1979 mL0.9895 mL1.9790 mL9.8949 mL
20 mM0.0989 mL0.4947 mL0.9895 mL4.9475 mL
50 mM0.0396 mL0.1979 mL0.3958 mL1.9790 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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