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Teneligliptin hydrobromide

现货
Catalog No.
A3865
DDP4抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,100.00
现货
10mg
¥ 550.00
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50mg
¥ 1,600.00
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100mg
¥ 2,400.00
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250mg
¥ 5,000.00
现货

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Background

Teneligliptin hydrobromide is a novel, potent, and long-lasting dipeptidyl peptidase-4 (DPP-4) inhibitor with antioxidant properties; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of about 1 nM[1].

DPP4 is also known as adenosine deaminase complexing protein 2 or CD26. DPP4 is an antigenic enzyme expressed on the membrane of most cell types and is associated with immune regulation, signal transduction and apoptosis [2].

In vitro: In human umbilical vein endothelial cells, Teneligliptin promoted the antioxidant response, reduced ROS levels and induced Nrf2-target genes messenger ribonucleic acid expression. Teneligliptin improved proliferation rates in HUVECs exposed to high glucose, regulating the expression of cell-cycle inhibitors markers (P21, P53 and P27), and reducing proapoptotic genes (BAX and CASP3), while promoteed BCL2 expression. Teneligliptin ameliorated high glucose-induced endoplasmic reticulum stress. Teneligliptin exihibited antioxidant properties and overcome the metabolic memory effect induced by chronic exposure to high glucose in HUVECs[3].

In vivo:In teneligliptin-treated mice, serum alanine aminotransferase and intrahepatic triglyceride levels were significantly decreased (p < 0.05). Teneligliptin also significantly downregulated hepatic mRNA levels of the genes involved in de novo lipogenesis (p < 0.05). Moreover, The hepatic expression levels of phosphorylated AMP-activated protein kinase (AMPK) protein were upregulated by teneligliptin[4]. Orally administration of teneligliptin at a dosage of 20 mg once daily in adults in the ovariectomized (OVX) mice maintained on a high-fat diet, teneligliptin effectively ameliorated the characteristics of metabolic abnormalities associated with postmenopausal obesity. Teneligliptin ameliorated the decreased energy consumption in the dark and light phases, reduced locomotor activity in the dark phase, and lowered core body temperature in OVX-HF[5].

References:
[1] Kishimoto M.  Teneligliptin: a DPP-4 inhibitor for the treatment of type 2 diabetes[J]. Diabetes, metabolic syndrome and obesity: targets and therapy, 2013, 6: 187.
[2] Kameoka J, Tanaka T, Nojima Y, et al.  Direct association of adenosine deaminase with a T cell activation antigen, CD26[J]. Science, 1993, 261(5120): 466-469.
[3] Pujadas G, De Nigris V, Prattichizzo F, et al.  The dipeptidyl peptidase-4 (DPP-4) inhibitor teneligliptin functions as antioxidant on human endothelial cells exposed to chronic hyperglycemia and metabolic high-glucose memory[J]. Endocrine, 2016: 1-12.
[4] Ideta T, Shirakami Y, Miyazaki T, et al.  The Dipeptidyl Peptidase-4 Inhibitor Teneligliptin Attenuates Hepatic Lipogenesis via AMPK Activation in Non-Alcoholic Fatty Liver Disease Model Mice[J]. International journal of molecular sciences, 2015, 16(12): 29207-29218.
[5] Sameshima A, Wada T, Ito T, et al.  Teneligliptin improves metabolic abnormalities in a mouse model of postmenopausal obesity[J]. Journal of Endocrinology, 2015, 227(1): 25-36.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt1257.72
Cas No.906093-29-6
FormulaC44H65Br5N12O2S2
Solubility≥62.9 mg/mL in DMSO, ≥12.1 mg/mL in EtOH with ultrasonic and warming, ≥104.8 mg/mL in H2O
Chemical Name[(2S,4S)-4-[4-(5-methyl-2-phenylpyrazol-3-yl)piperazin-1-yl]pyrrolidin-2-yl]-(1,3-thiazolidin-3-yl)methanone;pentahydrobromide
SDFDownload SDF
Canonical SMILESCC1=NN(C(=C1)N2CCN(CC2)C3CC(NC3)C(=O)N4CCSC4)C5=CC=CC=C5.CC1=NN(C(=C1)N2CCN(CC2)C3CC(NC3)C(=O)N4CCSC4)C5=CC=CC=C5.Br.Br.Br.Br.Br
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

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化学结构

Teneligliptin hydrobromide