Teneligliptin Hydrobromide Hydrate Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 2 mg/ml; PBS (pH 7.2): 10 mg/ml

form 

A crystalline solid

color 

White to off-white

InChIKey

IBFYBPDPBLVHHZ-RPZAKFRXNA-N

SMILES

CC1=NN(C2C=CC=CC=2)C(N2CCN([C@@H]3CN[C@H](C(N4CSCC4)=O)C3)CC2)=C1.Br.O |&1:15,18,r|

Teneligliptin Hydrobromide Hydrate Usage And Synthesis

Uses

Teneligliptin (MP-513) hydrobromide hydrate is an orally active and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50s: 0.37 and 0.29 nM for the human and rat DPP-4, respectively). Teneligliptin hydrobromide hydrate improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus[1][2][3][4][5][6][7][8].

IC 50

TLR4; NLRP3 inflammasome; DPP-4

References

[1] Fukuda-Tsuru S, et al. A novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor, teneligliptin, improves postprandial hyperglycemia and dyslipidemia after single and repeated administrations. Eur J Pharmacol. 2012 Dec 5;696(1-3):194-202. DOI:10.1016/j.ejphar.2012.09.024
[2] Yoshida T, et al. 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. Bioorg Med Chem. 2012 Oct 1;20(19):5705-19. DOI:10.1016/j.bmc.2012.08.012
[3] Guo D, et al. Beneficial effects of combination therapy of canagliflozin and teneligliptin on diabetic polyneuropathy and β-cell volume density in spontaneously type 2 diabetic Goto-Kakizaki rats. Metabolism. 2020 Jun;107:154232. DOI:10.1016/j.metabol.2020.154232
[4] Zhang GL, et al. Teneligliptin mitigates diabetic cardiomyopathy by inhibiting activation of the NLRP3 inflammasome. World J Diabetes. 2024 Apr 15;15(4):724-734. DOI:10.4239/wjd.v15.i4.724
[5] Fukuda-Tsuru S, et al. The novel dipeptidyl peptidase-4 inhibitor teneligliptin prevents high-fat diet-induced obesity accompanied with increased energy expenditure in mice. Eur J Pharmacol. 2014 Jan 15;723:207-15. DOI:10.1016/j.ejphar.2013.11.030
[6] Zhang Z, et al. Teneligliptin protects against hypoxia/reoxygenation-induced endothelial cell injury. Biomed Pharmacother. 2019 Jan;109:468-474. DOI:10.1016/j.biopha.2018.10.016
[7] Peng W, et al. Teneligliptin prevents doxorubicin-induced inflammation and apoptosis in H9c2 cells. Arch Biochem Biophys. 2020 Apr 15;683:108238. DOI:10.1016/j.abb.2019.108238
[8] Liu X, et al. Teneligliptin inhibits lipopolysaccharide-induced cytotoxicity and inflammation in dental pulp cells. Int Immunopharmacol. 2019 Aug;73:57-63. DOI:10.1016/j.intimp.2019.04.059
[9] Elumalai S, et al. High glucose-induced PRDX3 acetylation contributes to glucotoxicity in pancreatic β-cells: Prevention by Teneligliptin. Free Radic Biol Med. 2020 Nov 20;160:618-629. DOI:10.1016/j.freeradbiomed.2020.07.030

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