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Gemigliptin

Cat. No. M20841
Gemigliptin Structure
Synonym:

Zemiglo, LC15-0444

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Biological Activity

Gemigliptin (Zemiglo, LC15-0444) is a potent, selective and long-acting dipeptidyl peptidase 4 (DPP 4) inhibitor with a Ki of 7.25 nM. Gemigliptin shows at least >23,000-fold selectivity for DPP-4 over various proteases and peptidases, including DPP-8, DPP-9, and fibroblast activation protein (FAP)-α.

Chemical Information
Molecular Weight 489.36
Formula C18H19F8N5O2
CAS Number 911637-19-9
Solubility (25°C) DMSO 98 mg/mL
Water 12 mg/mL
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] Giang Nguyen, et al. Endocrinol Metab (Seoul). Gemigliptin Alleviates Succinate-Induced Hepatic Stellate Cell Activation by Ameliorating Mitochondrial Dysfunction

[2] Nami Lee, et al. J Immunol Res. Anti-inflammatory Effects of Empagliflozin and Gemigliptin on LPS-Stimulated Macrophage via the IKK/NF- κ B, MKK7/JNK, and JAK2/STAT1 Signalling Pathways

[3] Wan Seok Kang, et al. Biomed Pharmacother. Gemigliptin suppresses salivary dysfunction in streptozotocin-induced diabetic rats

[4] Oak-Kee Hong, et al. Endocrinol Metab (Seoul). Gemigliptin Inhibits Interleukin-1β-Induced Endothelial-Mesenchymal Transition via Canonical-Bone Morphogenetic Protein Pathway

[5] Manish Gutch, et al. Indian J Endocrinol Metab. Gemigliptin: Newer Promising Gliptin for Type 2 Diabetes Mellitus

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Keywords: Gemigliptin, Zemiglo, LC15-0444 supplier, DPP, inhibitors, activators


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