Sitagliptin phosphate monohydrate

Catalog No.S4002 Synonyms: MK-0431

Sitagliptin phosphate monohydrate Chemical Structure

Molecular Weight(MW): 523.32

Sitagliptin phosphate monohydrate is a potent inhibitor of DPP-IV with IC50 of 19 nM in Caco-2 cell extracts.

Size Price Stock Quantity  
In DMSO USD 120 In stock
USD 90 In stock
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2 Customer Reviews

  • AR staining of non-CAVD and CAVD patient hVICs in the presence or absence of Sitagliptin (100 μM) after 4 weeks of osteogenic stimulation. The bar graph presents the AR-positive area measured in each culture dish.

    Circulation, 2017, 135(20):1935-1950. Sitagliptin phosphate monohydrate purchased from Selleck.

    Functional lack of DPP4 activity was confirmed in plasma samples from DPP4mut rats, as compared to DAwt (E, white and dark bars) and to rats treated with sitagliptin for three weeks (E, light gray bars). Specificity of the assay was further confirmed by inhibition of the measured peptidase activity with sitagliptin, in vitro.

    Psychoneuroendocrinology, 2015, 53:195—206. Sitagliptin phosphate monohydrate purchased from Selleck.

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Biological Activity

Description Sitagliptin phosphate monohydrate is a potent inhibitor of DPP-IV with IC50 of 19 nM in Caco-2 cell extracts.
Features A potent, orally active inhibitor of DPP-4.
Targets
DPP-4 [1]
(Cell-free assay)
19 nM
In vitro

As an orally active agent, Sitagliptin phosphate exhibits a potent inhibitory effect on DPP-4 with IC50 of 19 nM from Caco-2 cell extracts. [1] MK0431 reduces in vitro migration of isolated splenic CD4 T-cells through a pathway involving cAMP/PKA/Rac1 activation. [2] A recent study demonstrates that sitagliptin exerts a novel, direct action in order to stimulate GLP-1 secretion by the intestinal L cell through a DPP-4-independent, protein kinase A- and MEK-ERK1/2-dependent pathway. It therefore reduces the effect of autoimmunity on graft survival. [3]

In vivo In vivo, the ED50 value of Sitagliptin phosphate for inhibition of plasma DPP-4 activity is calculated to be 2.3 mg/kg 7 hour postdose and 30 mg/kg 24 hour postdose in freely fed Han-Wistar rats. [1] The streptozotocin-induced type 1 diabetes mouse model exhibits elevated DPP-4 levels in the plasma that can be substantially inhibited in mice on an Sitagliptin phosphate diet. This is achieved by a positive effect on the regulation of hyperglycemia, potentially through prolongation of islet graft survival. [4] The plasma clearance and volume of distribution of Sitagliptin phosphate are higher in rats (40-48 mL/min/kg, 7-9 L/kg) than in dogs (9 mL/min/kg, 3 L/kg); and its half-life is shorter in rats,2 hours compared with 4 hours in dogs. [5]

Protocol

Kinase Assay:[1]
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Plasma DPP-4 Activity[2] :

DPP-4 is extracted from confluent Caco-2 cells. After 5 minutes of incubation at room temperature with lysis buffer (10 mM Tris-HCl, 150 mM NaCl, 0.04 U/mL aprotinin, 0.5% Nonidet P40, pH 8.0), cells are centrifuged at 35,000 g at 4 °C for 30 minutes, and the supernatant is stored at -80°C. Assays are performed by mixing 20 μL of appropriate compound dilutions with 50 μL of the substrate for the DPP-4 enzyme, H-Ala-Pro-7-amido-4-trifluoromethylcoumarin (final concentration in the assay, 100 μM) and 30 μL of the Caco-2 cell extract (diluted 1000-fold with 100 mM Tris-HCl, 100 mM NaCl, pH 7.8). Plates are incubated at room temperature for 1 hour, and fluorescence is measured at excitation/emission wavelengths of 405/535 nm using a SpectraMax GeminiXS. Dissociation kinetics of inhibitors from the DPP-4 enzyme is determined after a 1-hour preincubation of Caco-2 cell extracts with high inhibitor concentrations (30 nM for BI 1356, 3 μM for vildagliptin). The enzymatic reaction is started by adding the substrate H-Ala-Pro-7-amido-4-trifluoromethylcoumarin after a 3000-fold dilution of the preincubation mixture with assay buffer. Under these conditions, the difference in DPP-4 activity at a certain time point in the presence or absence of an inhibitor reflects the amount of this inhibitor still bound to the DPP-4 enzyme. Maximal reaction rates (fluorescence units/seconds × 1000) at 10-minute intervals are calculated using the SoftMax software of the SpectraMax and corrected for the rate of an uninhibited reaction [(vcontrol-vinhibitor)/vcontrol].
Cell Research:[2]
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  • Cell lines: CD4 T-cells
  • Concentrations: 100 μM
  • Incubation Time: 1 hour
  • Method: CD4T-cells are plated on membrane inserts in serum-free RPMI 1640, and cell migration is assayed using Transwell chambers (Corning), in the presence or absence of purified porcine kidney DPP-4 (32.1 units/mg; 100 mU/mL final concentration) and DPP-4 inhibitor (100 μM). After 1 hour, cells on the upper surface are removed mechanically, and cells that have migrated into the lower compartment are counted. The extent of migration is expressed relative to the control sample.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Freely fed Han-Wistar rats
  • Formulation: 0.5% aqueous hyroxyethylcellulose.
  • Dosages: ≤10 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (191.08 mM)
Water 41 mg/mL (78.34 mM)
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
Saline
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 523.32
Formula

C16H15F6N5O.H3PO4.H2O

CAS No. 654671-77-9
Storage powder
Synonyms MK-0431

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02363335 Completed Healthy Volunteers National Institute on Aging (NIA)|National Institutes of Health Clinical Center (CC) January 26, 2015 Phase 1
NCT02689362 Not yet recruiting Diabetes Mellitus, Type 2 Eurofarma Laboratorios S.A. March 2017 Phase 2
NCT02917031 Recruiting Type 2 Diabetes Mellitus|Heart Failure AstraZeneca January 2017 Phase 4
NCT02882477 Not yet recruiting Diabetes Mellitus|Iron Metabolism Disorders|Gastroduodenal Ulcer|Optic Atrophy|Sensorineural Hearing Loss|Platelet Dysfunction Hadassah Medical Organization December 2016 Phase 2|Phase 3
NCT02956044 Recruiting Type2 Diabetes Mellitus Theracos November 2016 Phase 1
NCT02920918 Recruiting Heart Failure, Systolic|Diabetes Mellitus, Type 2 Virginia Commonwealth University|Janssen Scientific Affairs, LLC October 2016 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID