Orlistat (Synonyms: 奥利司他; Tetrahydrolipstatin; Ro-18-0647)

目录号: HY-B0218 纯度: 99.97%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Orlistat (Tetrahydrolipstatin) 是一种不可逆的胰腺和胃脂肪酶 (lipases) 抑制剂。 Orlistat也是一种脂肪酸合成酶 (FASN) 抑制剂，口服用于肥胖症的长期研究。具有抗动脉粥样硬化作用。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Orlistat Chemical Structure

CAS No. : 96829-58-2

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥992	In-stock
100 mg	￥902	In-stock
200 mg	￥1560	In-stock
500 mg	￥2768	In-stock
1 g		询价
5 g		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Orlistat:

Orlistat (Standard) In-stock
Orlistat-d₃ 询价

MCE 顾客使用本产品发表的 14 篇科研文献

: Orlistat purchased from MCE. Usage Cited in: Nutrients. 2018 Mar 15;10(3). pii: E353. [Abstract]; Treatment with Orlistat leads to increased phospho-ACC without affecting the phosphorylation status of TOPK/survivin.

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生物活性
纯度 & 产品资料
参考文献

生物活性

Orlistat (Tetrahydrolipstatin) is a well-known irreversible inhibitor of pancreatic and gastric lipases. Orlistat is also an inhibitor of fatty acid synthase (FASN), is used orally for long-term research of obesity^[1]. Anti-atherosclerotic effect^[2].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BXPC-3	IC₅₀	8.45 μM Compound: Orlistat	Inhibition of survival of human BxPC3 cells after 10 to 14 days by crystal violet staining-based colony formation assay Inhibition of survival of human BxPC3 cells after 10 to 14 days by crystal violet staining-based colony formation assay	[PMID: 25513712]
COS-7	IC₅₀	1 μM Compound: 1, THL	Inhibition of human recombinant DAGL-alpha-mediated sn-1-[14C]oleoyl-2-arachidonoyl-glycerol hydrolysis to 2-AG overexpressed in african green monkey COS7 cell membrane by scintillation counting Inhibition of human recombinant DAGL-alpha-mediated sn-1-[14C]oleoyl-2-arachidonoyl-glycerol hydrolysis to 2-AG overexpressed in african green monkey COS7 cell membrane by scintillation counting	[PMID: 18831576]
HEK293	IC₅₀	0.19 μM Compound: THL, orlistat	Inhibition of human ABHD12 expressed in HEK293 cells pre-incubated for 10 mins before 2-AG substrate addition by HPLC method Inhibition of human ABHD12 expressed in HEK293 cells pre-incubated for 10 mins before 2-AG substrate addition by HPLC method	[PMID: 26344596]
HEK-293T	IC₅₀	> 100 μM Compound: THL	Inhibition of recombinant KIAA1363 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe Inhibition of recombinant KIAA1363 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe	[PMID: 18657971]
HEK-293T	IC₅₀	> 100 μM Compound: THL	Inhibition of recombinant FAAH transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe Inhibition of recombinant FAAH transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe	[PMID: 18657971]
HEK-293T	IC₅₀	0.03 μM Compound: THL	Inhibition of recombinant BAT5 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe Inhibition of recombinant BAT5 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe	[PMID: 18657971]
HEK-293T	IC₅₀	0.05 μM Compound: THL	Inhibition of recombinant PLA2g7 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe Inhibition of recombinant PLA2g7 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe	[PMID: 18657971]
HEK-293T	IC₅₀	0.08 μM Compound: THL	Inhibition of recombinant ABHD12 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe Inhibition of recombinant ABHD12 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe	[PMID: 18657971]
HEK-293T	IC₅₀	10 nM Compound: 3, THL	Inhibition of human DAGLalpha expressed in HEK293T cell membrane using [14C]SAG substrate in detergent free solution by FRET assay Inhibition of human DAGLalpha expressed in HEK293T cell membrane using [14C]SAG substrate in detergent free solution by FRET assay	[PMID: 22738638]
HepG2	EC₅₀	28.2 μM Compound: Orlistat	Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis	[PMID: 20966043]
MCF7	IC₅₀	> 1 x 10⁵ nM Compound: 1; THL	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29541373]
MDA-MB-231	IC₅₀	> 1 x 10⁵ nM Compound: 1; THL	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29541373]
MDA-MB-435	IC₅₀	16.8 μM Compound: orlistat	Cytotoxicity against human MDA-MB-435 cells after 48 hrs by Cell titer assay Cytotoxicity against human MDA-MB-435 cells after 48 hrs by Cell titer assay	[PMID: 18710210]
NCI-H460	IC₅₀	> 1 x 10⁵ nM Compound: 1; THL	Cytotoxicity against human H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29541373]
PANC-1	IC₅₀	203 μM Compound: Orlistat	Inhibition of FASN in human PANC1 cells assessed as inhibition of [14C]acetate incorporation preincubated for 4 hrs before [14C]acetate addition measured after 2 hrs by scintillation counting Inhibition of FASN in human PANC1 cells assessed as inhibition of [14C]acetate incorporation preincubated for 4 hrs before [14C]acetate addition measured after 2 hrs by scintillation counting	[PMID: 25513712]

体外研究
(In Vitro)

Orlistat (40 μM；2 天) 不影响人黑色素瘤细胞系中的 MGMT 水平，但在人外周血单核细胞、两种白血病和两种结肠癌细胞系中下调修复蛋白 30-70%。Orlistat 不会显著改变 MGMT mRNA 表达^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	The human melanoma cell line M10, Peripheral blood mononuclear cells , The human Jurkat CD4⁺ T cell leukemia cell line, the human promyelocytic leukemia cell line HL-60, the epithelial colon cancer HCT116 cells,non adherent mononuclear cells (NAMNC)^[1]
Concentration:	2.5, 5, 10, 20, 40 μM for Jurkat cells; 20 and 40 μM for HCT116 cells; 40 μM for normal NAMNC, M10 melanoma, HL-60 promyelocytic leukemia, and HT-29 colon cancer cells
Incubation Time:	2 days for Jurkat cells; 2 or 4 days for HCT116 cells; 2 days for NAMNC, M10 melanoma, HL-60 promyelocytic leukemia, HT-29 colon cancer
Result:	Reduced by >50% the MGMT level at the concentration of 40 μM for Jurkat cells, whereas little or no effect was found when lower concentrations were used. Downregulation of MGMT expression is produced at 40 μM for HCT116 cells. Provoked an ~50% reduction of MGMT level at 40 μM in normal NAMNC, and HL-60 promyelocytic leukemia, HT-29 colon cancer cells except for melanoma M10 cells that showed no downregulation of the protein.

体内研究
(In Vivo)

与肥胖 (OB) 组相比，Orlistat (10 mg/kg/天) 显著改善血脂状况，增加抗氧化酶和抗炎标志物的表达，并降低促炎标志物的表达^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Eighteen male rats of Sprague–Dawley strain aged between 8–10 weeks weighing 200-250 g^[2]
Dosage:	10 mg/kg/day
Administration:	Orally; six weeks
Result:	Treatment persistently restored the increased body weight, which was significantly observed at the ninth week until the end of the experimental period.

Clinical Trial

分子量

495.73

Formula

C₂₉H₅₃NO₅

CAS 号

96829-58-2

性状

固体

颜色

White to off-white

中文名称

奥利司他

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (201.72 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0172 mL	10.0861 mL	20.1723 mL
5 mM	0.4034 mL	2.0172 mL	4.0345 mL
10 mM	0.2017 mL	1.0086 mL	2.0172 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.04 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.04 mM); 悬浊液; 超声助溶

此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.04 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.97%

选择批次：

Data Sheet (642 KB) SDS (393 KB)

COA (289 KB) HNMR (289 KB) RP-HPLC (211 KB) MS (69 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Giorgia Cioccoloni, 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. [Content Brief]

[2]. Zaidatul Akmal Othman, et al. Anti-Atherogenic Effects of Orlistat on Obesity-Induced Vascular Oxidative Stress Rat Model. Antioxidants (Basel). 2021 Feb 6;10(2):251. [Content Brief]

Orlistat 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0172 mL	10.0861 mL	20.1723 mL	50.4307 mL
	5 mM	0.4034 mL	2.0172 mL	4.0345 mL	10.0861 mL
	10 mM	0.2017 mL	1.0086 mL	2.0172 mL	5.0431 mL
	15 mM	0.1345 mL	0.6724 mL	1.3448 mL	3.3620 mL
	20 mM	0.1009 mL	0.5043 mL	1.0086 mL	2.5215 mL
	25 mM	0.0807 mL	0.4034 mL	0.8069 mL	2.0172 mL
	30 mM	0.0672 mL	0.3362 mL	0.6724 mL	1.6810 mL
	40 mM	0.0504 mL	0.2522 mL	0.5043 mL	1.2608 mL
	50 mM	0.0403 mL	0.2017 mL	0.4034 mL	1.0086 mL
	60 mM	0.0336 mL	0.1681 mL	0.3362 mL	0.8405 mL
	80 mM	0.0252 mL	0.1261 mL	0.2522 mL	0.6304 mL
	100 mM	0.0202 mL	0.1009 mL	0.2017 mL	0.5043 mL

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Orlistat (Synonyms: 奥利司他; Tetrahydrolipstatin; Ro-18-0647)

Customer Review

Other Forms of Orlistat:

MCE 顾客使用本产品发表的 14 篇科研文献