Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | 2C22H30N6OS.5BrH |
| Molecular Weight | 1257.716 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Br.Br.Br.Br.Br.[H][C@]1(CN[C@@]([H])(C1)C(=O)N2CCSC2)N3CCN(CC3)C4=CC(C)=NN4C5=CC=CC=C5.[H][C@]6(CN[C@@]([H])(C6)C(=O)N7CCSC7)N8CCN(CC8)C9=CC(C)=NN9C%10=CC=CC=C%10
InChI
InChIKey=LUXIOMHUGCXFIU-MAYGPZJUSA-N
InChI=1S/2C22H30N6OS.5BrH/c2*1-17-13-21(28(24-17)18-5-3-2-4-6-18)26-9-7-25(8-10-26)19-14-20(23-15-19)22(29)27-11-12-30-16-27;;;;;/h2*2-6,13,19-20,23H,7-12,14-16H2,1H3;5*1H/t2*19-,20-;;;;;/m00...../s1
DescriptionCurator's Comment: description was created based on several sources, including https://www.pmda.go.jp/files/000153594.pdf
Curator's Comment: description was created based on several sources, including https://www.pmda.go.jp/files/000153594.pdf
Teneligliptin is a DPP IV inhibitor which was developed by Mitsubishi Tanabe Pharma and now is used for the treatment of type 2 diabetes mellitus in Asia under the name Tenelia.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. | 2012 Oct 1 |
|
| Teneligliptin: a DPP-4 inhibitor for the treatment of type 2 diabetes. | 2013 |
|
| Efficacy and safety of teneligliptin in combination with pioglitazone in Japanese patients with type 2 diabetes mellitus. | 2013 Nov 27 |
|
| Efficacy, safety and dose-response relationship of teneligliptin, a dipeptidyl peptidase-4 inhibitor, in Japanese patients with type 2 diabetes mellitus. | 2013 Sep |
|
| Comparative Binding Analysis of Dipeptidyl Peptidase IV (DPP-4) with Antidiabetic Drugs - An Ab Initio Fragment Molecular Orbital Study. | 2016 |
Sample Use Guides
The usual adult dosage is 20 mg of teneligliptin administered orally once daily. If efficacy is insufficient, the dose may be increased up to 40 mg once daily while closely monitoring the clinical course.
Route of Administration:
Oral
Human umbilical vein endothelial cells were cultured under normal (5 mmol/L) or high glucose level (25 mmol/L) during 21 days, or at high glucose during 14 days followed by 7 days at normal glucose, to reproduce the high-metabolic memory state. At this time, different concentrations of teneligliptin (0.1, 1.0 and 3.0 umol/L) were added to cells. Teneligliptin was shown to protect human umbilical vein endothelial cells from oxidative stress.
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DTXSID90238219
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ACTIVE MOIETY
SUBSTANCE RECORD
