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Sitagliptin phosphate monohydrate

Cat. No. M1967
Sitagliptin phosphate monohydrate Structure
Synonym:

MK-0431, Januvia

Size Price Availability Quantity
200mg USD 75 In stock
1g USD 220 In stock
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Quality Control
Biological Activity

Sitagliptin phosphate monohydrate is an oral antihyperglycemic (antidiabetic drug) of the dipeptidyl peptidase-4 (DPP-4) inhibitor class. Sitagliptin phosphate works to competitively inhibit the enzyme dipeptidyl peptidase 4 (DPP-4). This enzyme breaks down the incretins GLP-1 and GIP, gastrointestinal hormones released in response to a meal. Sitagliptin phosphate monohydrate has been shown to lower HbA1c level by about 0.7% points versus placebo. Sitagliptin phosphate is slightly less effective than metformin when used as a monotherapy and does not cause a weight gain compared to sulfonylureas. Sitagliptin phosphate (MK-0431) reduces in vitro migration of isolated splenic CD4 T-cells through a pathway involving cAMP/PKA/Rac1 activation. The ED50 value of Sitagliptin phosphate for inhibition of plasma DPP-4 activity is 30 mg/kg 24 hour postdose in vivo. Sitagliptin phosphate monohydrate is used for treatment of diabetes mellitus type 2.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 523.32
Formula C16H15F6N5O.H3PO4.H2O
CAS Number 654671-77-9
Purity >99%
Solubility DMSO 100 mg/mL
Water 100 mg/mL
Storage at -20°C
References

Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects.
Herman GA, et al. J Clin Pharmacol. 2006 Aug;46(8):876-86. PMID: 16855072.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Sitagliptin phosphate monohydrate, MK-0431, Januvia supplier, DPP-4, inhibitors

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