Sitagliptin phosphate monohydrate

This product is for research use only, not for human use. We do not sell to patients.

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Size	Price	Stock
10g	$500	Check With Us
25g	$950	Check With Us
50g	$1425	Check With Us

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Cat #: V0741 CAS #: 654671-77-9 Purity ≥ 98%

Description: Sitagliptin phosphate (formerly also known as MK-431; trade name Januvia; Xelevia; Janumet) monohydrate, the phosphate and hydrated form of Sitagliptin which is an antihyperglycemic agent and antidiabetic drug, is a potent, triazolopyrazine-based, and orally bioavailable inhibitor of DPP-IV (dipeptidyl peptidase-4) with IC50 of 19 nM in Caco-2 cell extracts.

References: 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 acti

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	523.32
Molecular Formula	C16H15F6N5O.H3PO4.H2O
CAS No.	654671-77-9
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 100 mg/mL (191.1 mM)r
	Water: 41 mg/mL (78.3 mM)r
	Ethanol: <1 mg/mL
Solubility In Vivo	Saline: 30 mg/mL
SMILES Code	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.[H]O[H]
Synonyms	MK 431; Sitagliptin Phosphate; MK-0431; MK0431; MK 0431;Sitagliptin Phosphate Monohydrate; MK-431; MK431; trade name: Januvia Xelevia Janumet

Protocol	In Vitro	Sitagliptin phosphate exhibits a potent inhibitory effect on DPP-4 with IC50 of 19 nM from Caco-2 cell extracts.
Protocol	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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	1.9109 mL	9.5544 mL	19.1088 mL	38.2175 mL
5mM	0.3822 mL	1.9109 mL	3.8218 mL	7.6435 mL
10mM	0.1911 mL	0.9554 mL	1.9109 mL	3.8218 mL
20mM	0.0955 mL	0.4777 mL	0.9554 mL	1.9109 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

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

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.