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奥利司他 /Orlistat {[allProObj[0].p_purity_real_show]}

货号:A512085 同义名: Tetrahydrolipstatin;Ro-18-0647 Ambeed 开学季,买赠积分,赢豪礼

Orlistat is an approved reversible general lipase inhibitor with IC50 of 122 ng/mL, used to treat obesity.

Orlistat 化学结构 CAS号:96829-58-2
Orlistat 化学结构
CAS号:96829-58-2
Orlistat 3D分子结构
CAS号:96829-58-2
Orlistat 化学结构 CAS号:96829-58-2
Orlistat 3D分子结构 CAS号:96829-58-2
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Orlistat 纯度/质量文件 产品仅供科研

货号:A512085 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Lipase 其他靶点 纯度
XEN445 +++

endothelial lipase, IC50: 0.237 μM

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JZL184 ++++

MAGL, IC50: 8 nM

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Tanshinone IIA {[allProObj[0].p_purity_real_show]}
Orlistat {[allProObj[0].p_purity_real_show]}
Atglistatin ++

ATGL, IC50: 0.7 μM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Orlistat 生物活性

靶点
  • Lipase

描述 Orlistat, an anti-obesity drug, is a potent and specific inhibitor of intestinal lipases. It inhibits gastric and pancreatic lipases in the lumen of the gastrointestinal tract to decrease systemic absorption of dietary fat. Orlistat treatment also results in modest improvements in total cholesterol, low-density lipoprotein, blood pressure, and fasting glucose and insulin concentrations[3]. The use of orlistat has been associated with rare cases of acute kidney injury. Orlistat has a beneficial effect on carbohydrate metabolism. Orlistat interferes with the absorption of many drugs (such as warfarin, amiodarone, ciclosporin and thyroxine as well as fat-soluble vitamins), affecting their bioavailability and effectiveness[4]. Orlistat, a lipase inhibitor, acts locally in the gastrointestinal tract. An extremely low degree of systemic absorption for orlistat when administered with a hypocaloric, well-balanced diet with 20% to 30% of calories derived from fat (50-80 gm). Systemic absorption of orlistat is negligible; at a clinically efficacious dose level, orlistat is unlikely to produce systemic lipase inhibition[5]. When orlistat was administered in the early stage of AKT/c-Met-triggered hepatocarcinogenesis, it resulted in the elimination of hepatic tumor burden. Mechanistically, orlistat efficiently elevated PTEN expression and suppressed AKT/SREBP1/FASN (fatty acid synthase) signaling both in vivo and in vitro, impairing AKT/c-Met-driven de novo lipogenesis and aberrant proliferation[6].

Orlistat 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
COS7 cells Function assay Inhibition of human recombinant DAGLalpha overexpressed in african green monkey COS7 cells, IC50=0.06 μM 18657971
HEK293T cell Function assay Inhibition of human DAGLalpha expressed in HEK293T cell membrane using [14C]SAG substrate in detergent free solution by FRET assay, IC50=0.01 μM 22738638
HepG2 (DPX-2) cells Function assay 24 h Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis, EC50=28.2 μM 20966043
MDA-MB-435 cells Cytotoxicity assay 48 h Cytotoxicity against human MDA-MB-435 cells after 48 hrs by Cell titer assay, IC50=16.8 μM 18710210

Orlistat 参考文献

[1]Cioccoloni G, Bonmassar L, et al. Influence of fatty acid synthase inhibitor orlistat on the DNA repair enzyme O6-methylguanine-DNA methyltransferase in human normal or malignant cells in vitro. Int J Oncol. 2015 Aug;47(2):764-72.

[2]Kridel SJ, Axelrod F, et al. Orlistat is a novel inhibitor of fatty acid synthase with antitumor activity. Cancer Res. 2004 Mar 15;64(6):2070-5.

[3]Heck AM, Yanovski JA, Calis KA. Orlistat, a new lipase inhibitor for the management of obesity. Pharmacotherapy. 2000 Mar;20(3):270-9

[4]Filippatos TD, Derdemezis CS, Gazi IF, Nakou ES, Mikhailidis DP, Elisaf MS. Orlistat-associated adverse effects and drug interactions: a critical review. Drug Saf. 2008;31(1):53-65

[5]Zhi J, Melia AT, Eggers H, Joly R, Patel IH. Review of limited systemic absorption of orlistat, a lipase inhibitor, in healthy human volunteers. J Clin Pharmacol. 1995 Nov;35(11):1103-8

[6]Zhang C, Sheng L, Yuan M, Hu J, Meng Y, Wu Y, Chen L, Yu H, Li S, Zheng G, Qiu Z. Orlistat delays hepatocarcinogenesis in mice with hepatic co-activation of AKT and c-Met. Toxicol Appl Pharmacol. 2020 Apr 1;392:114918

Orlistat 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.02mL

0.40mL

0.20mL

10.09mL

2.02mL

1.01mL

20.17mL

4.03mL

2.02mL

Orlistat 技术信息

CAS号96829-58-2
分子式C29H53NO5
分子量 495.735
别名 Tetrahydrolipstatin;Ro-18-0647;Orlistat, Alli, Tetrahydrolipastatin, Tetrahydrolipstatin, THLP, Xenical;(–)-Tetrahydrolipstatin;Ro 18-0647/002
运输蓝冰
存储条件

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(211.81 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

5% DMSO+40% PEG 300+5% Tween 80+water 13 mg/mL

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