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Evogliptin tartrate

Cat. No. M27970
Evogliptin tartrate Structure
Synonym:

DA-1229 tartrate

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Quality Control & Documentation
Biological Activity

Evogliptin (DA-1229) tartrate is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin tartrate also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin tartrate can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation.

Chemical Information
Molecular Weight 551.51
Formula C23H32F3N3O9
CAS Number 1222102-51-3
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage 4°C, dry, sealed
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] Dong Han Won, et al. Int J Pharm. Active coating of immediate-release evogliptin tartrate to prepare fixed dose combination tablet with sustained-release metformin HCl

[2] Dong Han Won, et al. Int J Pharm. Optimization of bilayer tablet manufacturing process for fixed dose combination of sustained release high-dose drυg and immediate release low-dose drυg based on quality by design (QbD)

[3] Hyunyee Yoon, et al. Anal Biochem. Optimization and validation of a fluorogenic dipeptidyl peptidase 4 enzymatic assay in human plasma

[4] Dae Young Lee, et al. J Toxicol Environ Health A. Absorption, metabolism, and excretion of [14C]evogliptin tartrate in male rats and dogs

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