| 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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| ln Vitro |
Gigliptin has an IC50 of 11.69 mM and suppresses the production of AGE-BSA in a dose-dependent manner[1]. With an IC50 of 1.39 mM, gigliptin dose-dependently inhibits the cross-linking of preformed AGE-BSA with rat tail tendon collagen[1]. Gigliptin's Ki is 7.25 nM, making it a competitive inhibitor[2].
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| ln Vivo |
AGE production and AGE cross-linking are inhibited in vivo by gemigliptin (100 mg/kg; ig; daily; for 12 weeks) [1]. In rats, dogs, and monkeys, gigliptin suppresses plasma DPP-4 activity in a dose-dependent manner [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: po (oral gavage) every day for 12 weeks Experimental Results: Circulating AGE levels in serum were Dramatically diminished by 44.5 %. |
| References |
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| Additional Infomation |
Gemigliptin is an organonitrogen compound and an organooxygen compound. It is functionally related to a beta-amino acid.
Gemigliptin is under investigation in Type 2 Diabetes Mellitus. Gemigliptin has been investigated for the treatment of Cancer and Cisplatin Adverse Reaction. Gemigliptin is an orally bioavailable inhibitor of the serine protease dipeptidyl peptidase 4 (DPP-4), with hypoglycemic and potential renoprotective activities. Upon administration, gemigliptin binds to DPP-4 and inhibits the breakdown of the incretin hormones, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). This prolongs incretin activity, increases postprandial insulin secretion from pancreatic beta cells, decreases glucagon secretion, delays gastric emptying and lowers blood glucose levels. In addition, gemigliptin exerts a renoprotective effect, probably through enhanced GLP-1 signaling, may prevent apoptosis and acute kidney injury induced by nephrotoxic agents, and may protect against diabetic nephropathy. |
| Molecular Formula |
C18H19N5O2F8
|
|---|---|
| Molecular Weight |
489.36296
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| Exact Mass |
489.141
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| CAS # |
911637-19-9
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| Related CAS # |
Gemigliptin tartrate;1374639-74-3
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| PubChem CID |
11953153
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| Appearance |
White to orange solid powder
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| LogP |
2.95
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
33
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| Complexity |
746
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1CC(CN(C1=O)C[C@H](CC(=O)N2CCC3=C(C2)N=C(N=C3C(F)(F)F)C(F)(F)F)N)(F)F
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| InChi Key |
ZWPRRQZNBDYKLH-VIFPVBQESA-N
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| InChi Code |
InChI=1S/C18H19F8N5O2/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/h9H,1-8,27H2/t9-/m0/s1
|
| 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
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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 |
| 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 : ~50 mg/mL (~102.17 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.11 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 (5.11 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 | 2.0435 mL | 10.2174 mL | 20.4349 mL | |
| 5 mM | 0.4087 mL | 2.0435 mL | 4.0870 mL | |
| 10 mM | 0.2043 mL | 1.0217 mL | 2.0435 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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