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  2. Metabolic Enzyme/Protease Apoptosis
  3. Fatty Acid Synthase (FASN) Apoptosis
  4. Orlistat

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

目錄號(hào): HY-B0218 純度: 99.97%
COA 產(chǎn)品使用指南

Orlistat (Tetrahydrolipstatin) 是一種不可逆的胰腺和胃脂肪酶 (lipases) 抑制劑。 Orlistat也是一種脂肪酸合成酶 (FASN) 抑制劑，口服用于肥胖癥的長(zhǎng)期研究。具有抗動(dòng)脈粥樣硬化作用。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Orlistat Chemical Structure

Orlistat Chemical Structure

CAS No. : 96829-58-2

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規(guī)格 價(jià)格 是否有貨 數(shù)量
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   詢價(jià)  
5 g   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Orlistat:

    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.

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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].

    細(xì)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]
    體外研究
    (In Vitro)

    Orlistat (40 μM；2 天) 不影響人黑色素瘤細(xì)胞系中的 MGMT 水平，但在人外周血單核細(xì)胞、兩種白血病和兩種結(jié)腸癌細(xì)胞系中下調(diào)修復(fù)蛋白 30-70%。Orlistat 不會(huì)顯著改變 MGMT mRNA 表達(dá)[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.
    體內(nèi)研究
    (In Vivo)

    與肥胖 (OB) 組相比，Orlistat (10 mg/kg/天) 顯著改善血脂狀況，增加抗氧化酶和抗炎標(biāo)志物的表達(dá)，并降低促炎標(biāo)志物的表達(dá)[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 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    奧利司他
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 100 mg/mL (201.72 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.04 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.04 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.97%

    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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
    Help & FAQs
    • Do most proteins show cross-species activity?

      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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    產(chǎn)品名稱：
    Orlistat
    目錄號(hào)：
    HY-B0218
    需求量：