Teneligliptin hydrobromide

产品描述
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.

更多产品信息，请点击：https://www.glpbio.cn/search.php?catalog=GC15576
原装进口,Teneligliptin hydrobromide,美国GlpBio品Pai大包装更优惠!
美国Glpbio是一家领先的小分子YZ剂、激活剂、化合物库、多肽和实验室试剂的供应商。公司经营范围广泛，产品涉及癌症、免疫学、神经科学、细胞凋亡、表观遗传学等20多个不同研究领域，拥有10000多种产品。总部位于美国加利福尼亚，营销网点遍及法国、德国、加拿大、日本、澳大利亚、新加坡、以色列等20多个国家地区，竭诚为各国的科研工作者提供优质的产品和专业的服务。

温馨提示：不可用于临床ZL。