|3-[[(2S,4S)-4-[4-(3-甲基-1-苯基-1H-吡唑-5-基)-1-哌嗪基]-2-吡咯烷基]羰基]-噻唑烷两倍半氢溴酸盐|CsnPharm

CAS No.: 906093-29-6

氢溴酸替格列汀 Catalog No. CSN17332

Synonyms: MP-513 hydrobromide;Teneligliptin Hydrobromide Anhydrous;Teneligliptin

Teneligliptin Hydrobromide is a DPP4 inhibitor with IC50 value of <1 nM. It is commonly used as an add on treatment when meformin is not achieving the expected glycemic goals.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 DPP4

IC50:1.4nM
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].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 0.7951 mL
- 3.9755 mL
- 7.9509 mL
- 5 mM
- 0.1590 mL
- 0.7951 mL
- 1.5902 mL
- 10 mM
- 0.0795 mL
- 0.3975 mL
- 0.7951 mL

技术信息

CAS号

906093-29-6

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C44H65Br5N12O2S2

运输

蓝冰

分子量

1257.72

别名

MP-513 hydrobromide;Teneligliptin Hydrobromide Anhydrous;Teneligliptin;Teneligliptin Hydrobromide(2:5);Teneligliptin. trade name Tenelia;Teneligliptin HBr

溶解度

DMSO	98.0 mg/mL (77.9 mM)
Ethanol	16.0 mg/mL (12.7 mM)

动物实验配方

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氢溴酸替格列汀 Catalog No. CSN17332

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