貨號	規格	價格	上海	北京	武漢	南京
S81088-10mg	99.8%	￥127.00 S81088-10mg ￥127.00 現貨	14 >10	-	-	-
S81088-100mg	99.8%	￥382.00 S81088-100mg ￥382.00 現貨	16 >10	-	-	-
S81088-1g	99.8%	￥550.00 S81088-1g ￥550.00 現貨	6 6	-	-	-
S81088-5g	≥99%	￥1660.00 S81088-5g ￥1660.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

Teneligliptin (MP-513) hydrobromide is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM.

產品描述：

靶點：

IC50: 1 nM (DPP4);Others;?Proteasome;?DPP-4

體內研究：

Oral administration of Teneligliptin (MP-513) in Wistar rats results in the inhibition of plasma DPP-4 with an ED50 of 0.41 mg/kg. Plasma DPP-4 inhibition is sustained even at 24 h after administration of Teneligliptin (MP-513). An oral carbohydrate-loading test in Zucker fatty rats shows that Teneligliptin (MP-513) at ≥0.1 mg/kg increases the maximum increase in plasmaglucagon-like peptide-1 and insulin levels, and reduces glucose excursions. This effect is observed over 12 h after a dose of 1 mg/kg. An oral fat-loading test in Zucker fatty rats also shows that Teneligliptin (MP-513) at 1 mg/kg reduces triglyceride and free fatty acid excursions. In Zucker fatty rats, repeated administration of Teneligliptin (MP-513) for two weeks reduces glucose excursions in the oral carbohydrate-loading test and decreased the plasma levels of triglycerides and free fatty acids under non-fasting conditions. Oral administration of Teneligliptin (MP-513) inhibits plasma DPP-4 in rats in a dose-dependent manner. The ED50 value for Teneligliptin (MP-513) is calculated to be 0.41 mg/kg, while those for Sitagliptin and Vildagliptin, 27.3 and 12.8 mg/kg, respectively. Teneligliptin (MP-513) improves the histopathological appearance of the liver and decreases intrahepatic triglyceride levels in an NAFLD model mouse, which is associated with downregulation of hepatic lipogenesis-related genes due to AMPK activation

參考文獻：

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. 2. Ideta T, et al. The Dipeptidyl Peptidase-4 Inhibitor Teneligliptin Attenuates Hepatic Lipogenesis via AMPK Activation in Non-Alcoholic Fatty Liver Disease Model Mice. Int J Mol Sci. 2015 Dec 8;16(12):29207-18.

溶解性：

Soluble in DMSO、H2O

保存條件：

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.59 ml	7.951 ml	15.902 ml
5 mM	0.318 ml	1.59 ml	3.18 ml
10 mM	0.159 ml	0.795 ml	1.59 ml
50 mM	0.032 ml	0.159 ml	0.318 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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Teneligliptin Hydrobromide (2:5)