| 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 |
| Targets |
IC50: 10.3 nM (human recombinant DPP-4)[2]
Dipeptidyl peptidase-4 (DPP-4) |
|---|---|
| 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].
Gemigliptin tartrate potently inhibits human recombinant DPP-4 with an IC50 of 10.3 nM and a Ki of 7.25 nM. It is highly selective for DPP-4 over DPP-8, DPP-9, and FAP-alpha (IC50s = 277.28 uM, etc.). It also exhibits potent anti-glycation properties, inhibiting AGE-BSA formation with an IC50 of 11.69 mM and pre-formed AGE cross-links with an IC50 of 1.39 mM. |
| 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].
Gemigliptin tartrate dose-dependently inhibits plasma DPP-4 activity in rats, dogs, and monkeys. Oral administration (100 mg/kg, daily for 12 weeks) inhibits AGEs formation and AGE cross-links in vivo. It is approved for clinical use as an oral antidiabetic drug in several countries, demonstrating efficacy in lowering blood glucose and HbA1c. |
| Enzyme Assay |
DPP-4 enzymatic activity is measured using a fluorogenic substrate, typically Gly-Pro-AMC. The compound is pre-incubated with the enzyme in an assay buffer (e.g., 50 mM Tris-HCl, pH 7.4) at 37degC for 10 minutes. Substrate is added, and the reaction proceeds for 30 minutes at 37degC. Fluorescence is measured (Ex/Em=380/460 nm) to calculate inhibition and IC50.
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| Cell Assay |
General cellular protocols for DPP-4 inhibitors may involve Caco-2 or L6 myotube cells. Cells are treated with the compound, and DPP-4 activity is measured in cell lysates or on the cell surface. GLP-1 levels in the culture supernatant can be measured by ELISA to assess functional efficacy, as DPP-4 is responsible for GLP-1 degradation.
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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. Standard in vivo models for DPP-4 inhibitors include oral glucose tolerance tests (OGTT) in normal or diabetic rodents. Gemigliptin is administered orally (e.g., 1-10 mg/kg) 30 minutes before glucose challenge. Blood glucose is measured at multiple time points. In chronic studies (e.g., Zucker diabetic fatty rats), the compound is given daily for 4-8 weeks. |
| ADME/Pharmacokinetics |
As an approved drug, gemigliptin has a well-characterized PK profile. It is rapidly absorbed after oral administration, with peak plasma concentrations (Cmax) reached within 0.5-2 hours (Tmax). It has a long terminal half-life (approx. 24-30 hours), allowing for once-daily dosing. The tartrate salt is used to enhance aqueous solubility.
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| Toxicity/Toxicokinetics |
As an approved drug, gemigliptin has been extensively evaluated for safety. In clinical trials, it has been generally well-tolerated with a low incidence of adverse events. Common side effects may include nasopharyngitis, headache, and gastrointestinal disturbances. It is not associated with the weight gain seen with some other antidiabetics.
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| References |
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| Additional Infomation |
Gemigliptin (LC15-0444) is an approved drug for the treatment of type 2 diabetes mellitus in countries including South Korea and India. It functions as a DPP-4 inhibitor, increasing the levels of incretin hormones (GLP-1, GIP) to enhance insulin secretion and suppress glucagon release. It is also being researched for its anti-glycation properties.
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| Molecular Formula |
C22H25F8N5O8
|
|---|---|
| Molecular Weight |
639.449833631516
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| Exact Mass |
639.157
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| Elemental Analysis |
C, 41.32; H, 3.94; F, 23.77; N, 10.95; O, 20.02
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| CAS # |
1374639-74-3
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| Related CAS # |
Gemigliptin;911637-19-9
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| PubChem CID |
60199080
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| Appearance |
Light yellow to orange solid powder
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
19
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
43
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| Complexity |
880
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| Defined Atom Stereocenter Count |
3
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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
|
| InChi Key |
DPEZWSNXONTJHT-NDAAPVSOSA-N
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| InChi Code |
InChI=1S/C18H19F8N5O2.C4H6O6/c19-16(20)3-1-12(32)31(8-16)6-9(27)5-13(33)30-4-2-10-11(7-30)28-15(18(24,25)26)29-14(10)17(21,22)23;5-1(3(7)8)2(6)4(9)10/h9H,1-8,27H2;1-2,5-6H,(H,7,8)(H,9,10)/t9-;1-,2-/m01/s1
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| Chemical Name |
1-[(2S)-2-amino-4-[2,4-bis(trifluoromethyl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]-4-oxobutyl]-5,5-difluoropiperidin-2-one;(2R,3R)-2,3-dihydroxybutanedioic acid
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| Synonyms |
Gemigliptin tartrate; 58M64DC7Z4; LC15-0444 tartrate; LC150444 tartrate; LC-150444 tartrate; RefChem:1085741; 1374639-74-3; Gemigliptin (tartrate); LC 150444; Gemigliptin tartrate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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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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