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Gosogliptin

Cat. No. M30759
Gosogliptin Structure
Synonym:

PF-00734200; PF-734200

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Quality Control & Documentation
Biological Activity

Gosogliptin is a potent and selective inhibitor of dipeptidyl peptidase-IV (DPP-IV).

Chemical Information
Molecular Weight 366.41
Formula C17H24F2N6O
CAS Number 869490-23-3
Form Solid
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] No authors listed. Dipeptidyl Peptidase-4 Inhibitors

[2] I N Tyurenkov, et al. Zh Nevrol Psikhiatr Im S S Korsakova. [Cerebroprotective activity of metformin, gosogliptin, citicoline and a novel GPR119 agonist in cerebral ischemia under experimental diabetes mellitus]

[3] Avivit Cahn, et al. Expert Opin Emerg Drugs. An update on DPP-4 inhibitors in the management of type 2 diabetes

[4] Chieko Muto, et al. Int J Clin Pharmacol Ther. The pharmacokinetics and pharmacodynamics of PF-00734200, a DPP-IV inhibitor, in healthy Japanese subjects

[5] Haiqing Dai, et al. Br J Clin Pharmacol. The pharmacokinetics of PF-734200, a DPP-IV inhibitor, in subjects with renal insufficiency

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Keywords: Gosogliptin, PF-00734200; PF-734200 supplier, Dipeptidyl Peptidase, inhibitors, activators


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