| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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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].
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|---|---|
| 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].
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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. |
| 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. |
| References |
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| Molecular Formula |
C23H32F3N3O9
|
|---|---|
| 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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