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Teneligliptin HBr

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Chemical Structure| 906093-29-6 同义名 : MP-513 hydrobromide;Teneligliptin hydrobromide anhydrous
CAS号 : 906093-29-6
货号 : A253925
分子式 : C44H65Br5N12O2S2
纯度 : 98%
分子量 : 1257.716
MDL号 : MFCD23098790
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(83.48 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 200 mg/mL(159.02 mM)
动物实验配方：
生物活性
描述 Dipeptidylpeptidase 4 (DPP4) belongs to the S9b gene family of postproline serine peptidases. It acts mostly as a secreted membrane protein, mediating the degradation and inactivation of glucagon-like peptide (GLP)-1 and gastric inhibitory protein (GIP)[3]. Teneligliptin is a DPP4 inhibitor for the treatment of type 2 diabetes. Teneligliptin inhibits human plasma DPP-4 activity and recombinant human DPP-4 activity in a concentration-dependent manner with IC50 of 1.75 nM and 0.889 nM, respectively[4]. In human umbilical vein endothelial cells exposed to high glucose, teneligliptin (0.1, 1.0 and 3.0 µM) promoted the antioxidant response, reduced ROS levels and induced Nrf2-target genes messenger ribonucleic acid expression. It also improved proliferation rates, regulated the expression of cell-cycle inhibitors markers (P53, P21 and P27), and reduced proapoptotic genes (BAX and CASP3), while promoted BCL2 expression[5]. Teneligliptin effectively ameliorated the characteristics of metabolic abnormalities associated with postmenopausal obesity in ovariectomized (OVX) mice maintained on a high-fat diet[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.80mL

0.16mL

0.08mL

3.98mL

0.80mL

0.40mL

7.95mL

1.59mL

0.80mL
参考文献

[1]Sameshima A, Wada T, et al. Teneligliptin improves metabolic abnormalities in a mouse model of postmenopausal obesity. J Endocrinol. 2015 Oct;227(1):25-36.

[2]Kishimoto M. Teneligliptin: a DPP-4 inhibitor for the treatment of type 2 diabetes. Diabetes Metab Syndr Obes. 2013 May 6;6:187-95.

[3]Huan Y, Jiang Q, Liu JL, Shen ZF. Establishment of a dipeptidyl peptidases (DPP) 8/9 expressing cell model for evaluating the selectivity of DPP4 inhibitors. J Pharmacol Toxicol Methods. 2015 Jan-Feb;71:8-12. doi: 10.1016/j.vascn.2014.11.002. Epub 2014 Nov 15. PMID: 25464020.

[4]Kishimoto M. Teneligliptin: a DPP-4 inhibitor for the treatment of type 2 diabetes. Diabetes Metab Syndr Obes. 2013 May 6;6:187-95. doi: 10.2147/DMSO.S35682. PMID: 23671395; PMCID: PMC3650886.

[5]Pujadas G, De Nigris V, Prattichizzo F, La Sala L, Testa R, Ceriello A. The dipeptidyl peptidase-4 (DPP-4) inhibitor teneligliptin functions as antioxidant on human endothelial cells exposed to chronic hyperglycemia and metabolic high-glucose memory. Endocrine. 2017 Jun;56(3):509-520. doi: 10.1007/s12020-016-1052-0. Epub 2016 Aug 16. PMID: 27530507; PMCID: PMC5435779.

[6]Sameshima A, Wada T, Ito T, Kashimura A, Sawakawa K, Yonezawa R, Tsuneki H, Ishii Y, Sasahara M, Saito S, Sasaoka T. Teneligliptin improves metabolic abnormalities in a mouse model of postmenopausal obesity. J Endocrinol. 2015 Oct;227(1):25-36. doi: 10.1530/JOE-15-0239. Epub 2015 Aug 11. PMID: 26264980.