2. Metabolic Enzyme/Protease Autophagy
  3. Dipeptidyl Peptidase Autophagy
  4. Sitagliptin phosphate monohydrate

Sitagliptin phosphate monohydrate  (Synonyms: MK-0431 phosphate monohydrate)

Cat. No.: HY-13749B Purity: 99.49%
COA Handling Instructions

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Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.

For research use only. We do not sell to patients.

Sitagliptin phosphate monohydrate Chemical Structure

Sitagliptin phosphate monohydrate Chemical Structure

CAS No. : 654671-77-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in Water USD 73 In-stock
Solid
100 mg USD 66 In-stock
200 mg USD 79 In-stock
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Based on 18 publication(s) in Google Scholar

Other Forms of Sitagliptin phosphate monohydrate:

Sitagliptin phosphate monohydrate Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

DPP-4

 

In Vitro

Sitagliptin phosphate exhibits a potent inhibitory effect on DPP-4 with IC50 of 19 nM from Caco-2 cell extracts[1].?Sitagliptin 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Sitagliptin phosphate monohydrate Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

523.32

Formula

C16H20F6N5O6P
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

[H]O[H].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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : ≥ 33 mg/mL (63.06 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9109 mL 9.5544 mL 19.1088 mL
5 mM 0.3822 mL 1.9109 mL 3.8218 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 50 mg/mL (95.54 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.49%

COA (252 KB) LCMS (269 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[2]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice: Overnight fasted C57BL/6J mice are challenged 45 min after compound administration with an oral glucose load (2 g/kg). Blood samples for glucose measurement are obtained by tail bleed predose and at serial time points after the glucose load. To evaluate the duration of the effect on glucose tolerance, vehicle or DPP-4 inhibitors are administered 16 h before the glucose challenge.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 1.9109 mL 9.5544 mL 19.1088 mL 47.7719 mL
5 mM 0.3822 mL 1.9109 mL 3.8218 mL 9.5544 mL
10 mM 0.1911 mL 0.9554 mL 1.9109 mL 4.7772 mL
15 mM 0.1274 mL 0.6370 mL 1.2739 mL 3.1848 mL
20 mM 0.0955 mL 0.4777 mL 0.9554 mL 2.3886 mL
25 mM 0.0764 mL 0.3822 mL 0.7644 mL 1.9109 mL
30 mM 0.0637 mL 0.3185 mL 0.6370 mL 1.5924 mL
40 mM 0.0478 mL 0.2389 mL 0.4777 mL 1.1943 mL
50 mM 0.0382 mL 0.1911 mL 0.3822 mL 0.9554 mL
60 mM 0.0318 mL 0.1592 mL 0.3185 mL 0.7962 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Sitagliptin phosphate monohydrate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Sitagliptin phosphate654671-77-9MK-0431 phosphateDipeptidyl PeptidaseAutophagyDPPInhibitorinhibitorinhibit

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