| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
IC50: 10.3 nM (human recombinant DPP-4)[2]
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| ln Vitro |
With an IC50 of 11.69 mM, gemigliptin tartrate dose-dependently inhibits the formation of AGE-BSA[1]. ..With a Ki of 7.25 nM, gemigliptin tartrate is a competitive DPP-4 inhibitor[2].
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| ln Vivo |
In vivo, the production of AGEs and AGE cross-links is inhibited by gemigliptin tartrate (100 mg/kg; ig; daily; for 12 weeks|1]. In rats, dogs, and monkeys, gemigliptin tartrate dose-dependently suppresses plasma DPP-4 activity[2].
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| Animal Protocol |
Animal/Disease Models: Male C57BL/KsJ-db/db mice (7 weeks old)[1]
Doses: 100 mg/kg Route of Administration: Oral gavage, daily, for 12 weeks Experimental Results: Dramatically decreased circulating AGE levels by 44.5% in serum. |
| References |
[1]. Jung E, et al. Gemigliptin, a novel dipeptidyl peptidase-4 inhibitor, exhibits potent anti-glycation properties in vitro and in vivo. Eur J Pharmacol. 2014 Dec 5;744:98-102.
[2]. Kim SH, et al. Pharmacological profiles of gemigliptin (LC15-0444), a novel dipeptidyl peptidase-4 inhibitor, in vitro and in vivo. Eur J Pharmacol. 2016 Oct 5;788:54-64. |
| Molecular Formula |
C22H25F8N5O8
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|---|---|
| Molecular Weight |
639.45
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| CAS # |
1374639-74-3
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| Related CAS # |
Gemigliptin;911637-19-9
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| SMILES |
FC1(CCC(N(C1)C[C@H](CC(N1CC2C(=C(C(F)(F)F)N=C(C(F)(F)F)N=2)CC1)=O)N)=O)F.O[C@@H](C(=O)O)[C@H](C(=O)O)O
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (156.38 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5638 mL | 7.8192 mL | 15.6384 mL | |
| 5 mM | 0.3128 mL | 1.5638 mL | 3.1277 mL | |
| 10 mM | 0.1564 mL | 0.7819 mL | 1.5638 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
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