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Acyltransferase

Acyltransferase相关产品(12)
货号 产品名 中文名称 产品描述
SJ-MX1041 PF-06424439 methanesulfonate

PF-06424439 methanesulfonate 是一种口服有效,选择性的咪唑并吡啶二酰基甘油酰基转移酶 2 (DGAT2) 抑制剂,IC50 是 14 nM,在 MGAT1-3 或 DGAT1 上没有表现出显着的活性。PF-06424439 methanesulfonate可以减少人肝细胞中甘油三酯的合成, 降低大鼠血脂异常模型中的血浆甘油三酯和胆固醇水平。

SJ-MX0441 A 922500 A 922500 (DGAT-1 Inhibitor 4a) 是一种有效,选择性和口服可用的二酰甘油酰基转移酶 1 (DGAT-1) 抑制剂,抑制小鼠和人 DGAT-1 的 IC50s 分别为 9,22 nM。
SJ-MX2801 T863 T863 is a inhibitor of diacylglycerol O-acyltransferase 1 (DGAT1). It is tested pre-clinically as a potential treatment for obesity.
SJ-MX3398 Pradigastat (LCQ-908) Pradigastat (LCQ-908) is a novel, potent and orally bioavailable diacylglycerol acyltransferase 1 (DGAT1) inhibitor being developed for the treatment of familial chylomicronemia syndrome. Familial chylomicronemia syndrome (FCS) is a rare lipid disease caused by complete lipoprotein lipase (LPL) deficiency resulting in fasting chylomicronemia and severe hypertriglyceridemia. Inhibition of diacylglycerol acyltransferase 1 (DGAT1), which mediates chylomicron triglyceride (TG) synthesis, is an attractive strategy to reduce TG levels in FCS .
SJ-MX3490 AZD7687 AZD7687 is a novel, potent, selective, reversible and pyrazinecarboxamide-based inhibitor of diacylglycerol acyltransferase 1 (DGAT1) with an IC50 value of 80 nM for hDGAT1. AZD7687 attenuates postprandial triacylglyceride excursion. AZD7687 markedly reduced postprandial TAG excursion with a steep concentration-effect relationship. Incremental TAG AUC (area under the serum concentration vs. time curve) following SMM 60% was decreased >75% from baseline at doses ≥5 mg (p < 0.0001 vs. placebo). Serum levels of diacylglycerol, specifically measured with mass spectrometry, did not increase after AZD7687 administration. Nausea, vomiting and diarrhoea were reported with increasing doses and they limited dose escalation. Lowering of SMM fat content to 45 or 30% in five cohorts gradually reduced the frequency of gastrointestinal symptoms at a given dose of AZD7687.
SJ-MX1560 RHC 80267 RHC 80267 (U-57908) 是一种有效的选择性二酰基甘油脂酶 (DAGL) 抑制剂 (对犬血小板的 IC50 为 4 μM)。RHC 80267 抑制胆碱酯酶活性,IC50 为 4 μM,从而增强了乙酰胆碱引起的松弛。RHC 80267 还抑制 COX 活性和磷脂酰胆碱的水解。
SJ-MX2841 2-Furoic acid 糠酸

 

2-Furoic acid is a heterocyclic carboxylic acid that is shown to be effective in lowering both serum cholesterol and serum triglyceride levels significantly in rats with an elevation of HDL cholesterol level at 20 mg/kg/day orally.

SJ-MX0647 Avasimibe 阿伐麦布 Avasimibe (CI-1011; PD-148515) 是一种有效的,具有口服活性的酰基辅酶 A:胆固醇酰基转移酶 (ACAT) 抑制剂,对 ACAT1 和 ACAT2 的 IC50 分别为 24 和 9.2 μM。Avasimibe 可用于前列腺癌的研究。
SJ-MX0660 OSMI-4 OSMI-4 是一种低纳摩尔的O-连接的N-乙酰半乳糖胺转移酶 (OGT) 的抑制剂,其在细胞中的EC50 值为3 μM。
SJ-MN0388 Xanthohumol 黄腐酚 Xanthohumol 是从啤酒花中分离到的黄酮类化合物,是 DGAT,COX-1 和 COX-2 的抑制剂,具有抗肿瘤,抗血管生成的作用。Xanthohumol 还具有抗牛病毒性腹泻病毒 (BVDV),鼻病毒,HSV-1,HSV-2 和巨细胞病毒 (CMV) 的抗病毒活性。Xanthohumol 在肿瘤细胞中可诱导生长阻滞和凋亡。
SJ-MX2405 PF-04620110 PF-04620110 是一种有效、选择性的,有口服活性的甘油二酯酰基转移酶 -1 (DGAT1) 抑制剂,IC50 值为 19 nM。
SJ-MX4189 Nevanimibe Nevanimibe (PD-132301) 是一种口服有效的,选择性酰基辅酶 A:胆固醇 O-酰基转移酶 1 (ACAT1) 抑制剂,EC50 为 9 nM。Nevanimibe 抑制 ACAT2,EC50 为 368 nM。Nevanimibe 诱导细胞凋亡 (apoptosis),并具有抗肾上腺皮质癌的潜力。