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| Targets |
DPP-4 (Dipeptidyl Peptidase-4, also known as CD26). Evogliptin tartrate is a potent, competitive, and reversible inhibitor of DPP-4. By blocking DPP-4 activity, it prevents the rapid degradation of the incretin hormones GLP-1 (glucagon-like peptide-1) and GIP (glucose-dependent insulinotropic polypeptide). Elevated GLP-1 and GIP levels lead to increased glucose-dependent insulin secretion from pancreatic beta-cells, suppressed glucagon release from alpha-cells, delayed gastric emptying, and reduced hepatic glucose production, resulting in improved glycemic control. Evogliptin exhibits a Ki of 0.98-1.2 nM for human DPP-4.
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| ln Vitro |
In PWM-induced H9 Th1 cells, evogliptin tartrate (2.49 mM; 12 h) can efficiently decrease the activity of the mDPP4 (membrane DPP4) enzyme [1]. In primary hepatocytes of ATG7f/f-Cre+ mice, evogliptin tartrate induces autophagy, which inhibits inflammatory and fibrotic signaling [2].
Evogliptin tartrate is a potent competitive inhibitor of human DPP-4 with an IC50 of 0.98-1.2 nM. It is highly selective for DPP-4 over DPP-8 and DPP-9 (6,000-7,900-fold selectivity), which is important because inhibition of DPP-8/9 has been associated with toxicity (alopecia, thrombocytopenia, and GI effects in preclinical species). It also inhibits membrane-bound DPP-4 (mDPP4) activity in PWM-stimulated lymphocytes. The compound shows negligible off-target activity against a panel of other serine proteases. |
| ln Vivo |
In HFD/STZ mice, evogliptin tartrate (100, 300 mg/kg; animal feed; once daily for 10 weeks) reduces insulin resistance and glucose intolerance [3].
In mouse models of type 2 diabetes (e.g., db/db mice, high-fat diet [HFD]-induced obese mice), oral Evogliptin tartrate (1-10 mg/kg once daily) produces significant and sustained reductions in fasting blood glucose, postprandial glucose, and HbA1c levels. It also increases plasma active GLP-1 and insulin levels, reduces body weight gain, and improves insulin sensitivity. Beyond glucose control, evogliptin tartrate attenuates the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy, suggesting a potential role in non-alcoholic fatty liver disease (NAFLD). |
| Enzyme Assay |
Cell-free DPP-4 enzyme inhibition is measured using a fluorometric assay. Recombinant human DPP-4 (0.1-0.5 mU) is incubated with varying concentrations of Evogliptin tartrate (0.001-1000 nM) in assay buffer (50 mM Tris-HCl pH 7.4, 50 mM NaCl, 1 mM EDTA, 0.01% Tween-20) for 10-30 minutes at 25degC. The reaction is initiated by adding a synthetic substrate (e.g., Gly-Pro-AMC or Ala-Pro-AFC, 50-100 microM). The hydrolysis of the substrate releases the fluorescent group AMC (7-amino-4-methylcoumarin), which is measured kinetically over 30-60 minutes (excitation 380 nm, emission 460 nm). The IC50 is calculated from dose-response curves. For selectivity assays, the same procedure is performed using recombinant human DPP-8 and DPP-9 enzymes.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: H9 Th1 cells (Pokeweed mitogen (PWM) induced) Tested Concentrations: 2.49 mM (1 µg/mL) Incubation Duration: 12 hrs (hours) Experimental Results: Effective inhibition of mDPP4 (membrane DPP4) at a certain dose ) activity-dependent manner, but did not affect the cytokine profile or cell viability in PWM-activated CD4+CD26+ H9 Th1 cells. L6 rat myoblasts (or human skeletal muscle cells) are cultured in DMEM with 10% FBS. To measure GLP-1 secretion, GLUTag cells (enteroendocrine L-cells) are seeded in 24-well plates and treated with varying concentrations of Evogliptin tartrate (0.1-1000 nM) for 2-4 hours. Cell culture supernatants are collected, and GLP-1 (active) levels are measured by ELISA. For cellular DPP-4 activity, cells (e.g., THP-1 monocytes, primary human lymphocytes) are lysed, and cell lysates (10-50 microg protein) are incubated with the fluorogenic substrate Gly-Pro-AMC in the presence or absence of the compound. The inhibition of cellular DPP-4 activity is measured as described above. Cytotoxicity is assessed by MTT or LDH release assays. |
| Animal Protocol |
Animal/Disease Models: Male ICR mouse (4 weeks old; HFD/STZ mouse model) [3].
Doses: 100, 300 mg/kg Route of Administration: Animal feed; one time/day for 10 weeks Experimental Results: Blood glucose levels diminished starting from the second week and continued during the 300 mg/kg treatment period until 10 weeks. HbA1c levels were Dramatically diminished at a dose of 300 mg/kg. Dramatically diminished 6-hour fasting blood glucose levels in a dose-dependent manner. Male db/db mice (C57BL/KsJ-db/db, 6-8 weeks old, 30-50 g) or HFD-induced obese mice are used. Animals are randomized (n=8-10 per group) based on baseline non-fasting blood glucose levels. Evogliptin tartrate (1-10 mg/kg) or vehicle (e.g., 0.5% methylcellulose) is administered orally once daily for 28 days. Blood glucose is measured weekly using a glucometer (tail vein). An oral glucose tolerance test (OGTT) is performed at the end of the treatment period: after an overnight fast, animals receive an oral glucose challenge (2 g/kg), and blood glucose is measured at 0, 15, 30, 60, and 120 minutes post-dose. Blood samples are also collected for plasma insulin, active GLP-1, and HbA1c measurements. Pancreatic islets are isolated for histology (insulin staining), and liver and adipose tissues are harvested for gene expression analysis (qPCR). |
| ADME/Pharmacokinetics |
Evogliptin is rapidly absorbed after oral administration, with an absolute bioavailability of approximately 70-80%. Peak plasma concentrations (Cmax) are reached within 1-2 hours (Tmax). The terminal half-life is 10-12 hours in humans, supporting once-daily dosing. It is metabolized primarily by CYP3A4, with minimal involvement of other CYP isoforms. The tartrate salt enhances aqueous solubility for formulation. Evogliptin is approximately 40-50% protein bound. No dose adjustment is required in mild-to-moderate renal impairment models.
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| Toxicity/Toxicokinetics |
Evogliptin is generally well tolerated in preclinical studies and clinical trials. The most common adverse events reported include nasopharyngitis, headache, and mild gastrointestinal discomfort (nausea, diarrhea). Due to its high selectivity for DPP-4 over DPP-8/9, evogliptin does not cause the alopecia, thrombocytopenia, or GI toxicity observed with non-selective DPP-4 inhibitors. No significant hepatotoxicity or cardiotoxicity has been reported.
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| References |
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| Additional Infomation |
Evogliptin tartrate (brand name Suganon™) was approved in South Korea in 2015 for the treatment of type 2 diabetes mellitus as monotherapy or in combination with metformin and SGLT2 inhibitors. It is not approved by the US FDA or EMA as of 2025. Evogliptin is known for its excellent DPP-4 selectivity and has demonstrated renoprotective effects independent of its glucose-lowering activity. It is a research tool for studying pleiotropic effects of DPP-4 inhibition, including anti-inflammatory and anti-fibrotic effects in NAFLD and cardiovascular disease models.
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| Molecular Formula |
C23H32F3N3O9
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|---|---|
| Molecular Weight |
551.510097503662
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| Exact Mass |
551.209
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| CAS # |
1222102-51-3
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| Related CAS # |
Evogliptin;1222102-29-5
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| PubChem CID |
135395528
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
38
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| Complexity |
692
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| Defined Atom Stereocenter Count |
4
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| SMILES |
FC1C=C(C(=CC=1C[C@H](CC(N1CCNC([C@H]1COC(C)(C)C)=O)=O)N)F)F.O[C@@H](C(=O)O)[C@H](C(=O)O)O
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| InChi Key |
RBBXDAJRSNHIJZ-DLDKMZOSSA-N
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| InChi Code |
InChI=1S/C19H26F3N3O3.C4H6O6/c1-19(2,3)28-10-16-18(27)24-4-5-25(16)17(26)8-12(23)6-11-7-14(21)15(22)9-13(11)20;5-1(3(7)8)2(6)4(9)10/h7,9,12,16H,4-6,8,10,23H2,1-3H3,(H,24,27);1-2,5-6H,(H,7,8)(H,9,10)/t12-,16-;1-,2-/m11/s1
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| Chemical Name |
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-[(2-methylpropan-2-yl)oxymethyl]piperazin-2-one;(2R,3R)-2,3-dihydroxybutanedioic acid
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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 (~181.32 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.53 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 (4.53 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8132 mL | 9.0660 mL | 18.1320 mL | |
| 5 mM | 0.3626 mL | 1.8132 mL | 3.6264 mL | |
| 10 mM | 0.1813 mL | 0.9066 mL | 1.8132 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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