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  1. Metabolic Enzyme/Protease
  2. Fatty Acid Synthase (FASN)
  3. C75

C75 是合成的脂肪酸合成酶 (FASN) 抑制劑。C75 抑制前列腺癌細(xì)胞 PC3 的 IC50 值為 35 μM。C75 是有效的 CPT1A 激活劑。

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C75 Chemical Structure

C75 Chemical Structure

CAS No. : 218137-86-1

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10 mM * 1 mL in DMSO ¥1211
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Customer Review

Other Forms of C75:

    C75 purchased from MCE. Usage Cited in: Cell Death Discov. 2022 Oct 28;8(1):431.  [Abstract]

    Cell Counting Kit-8 (CCK8) assay. NUPR1 overexpression-induced proliferation of MHCC-97H and SK-Hep1 cells can be reversed by C75 (50 μM; 48 h).

    C75 purchased from MCE. Usage Cited in: Cell Death Discov. 2022 Oct 28;8(1):431.  [Abstract]

    Transwell migration assay. C75 reduces the migration ability of NUPR1-overexpressing SK-Hep1 cells.

    C75 purchased from MCE. Usage Cited in: Am J Cancer Res. 2020 Feb 1;10(2):595-609.  [Abstract]

    Of the transcription of spliced X-box-binding protein 1 (sXBP1) and phosphorylated translational initiation factor 2 in eukaryotes (eIF2α) are higher in ANGTPL4-/- macrophages but are restored to normal levels following C75 treatment.
    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    C75 is a synthetic fatty-acid synthase (FASN) inhibitor; inhibits prostate cancer cells PC3 with an IC50 of 35 μM[1][2][3]. C75 is a potent CPT1A activator[5].

    IC50 & Target

    IC50: 35 μM (PC3 cell)[1]

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    Fibroblast IC50
    63.2 μM
    Compound: (+/-)-C-75
    Antiproliferative activity against fibroblasts (unknown origin) after 72 hrs by MTT assay
    Antiproliferative activity against fibroblasts (unknown origin) after 72 hrs by MTT assay
    [PMID: 28324785]
    HCT-116 IC50
    46.4 μM
    Compound: (+/-)-C-75
    Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
    [PMID: 28324785]
    Huh-7 CC50
    > 100 μM
    Compound: 68
    Cytotoxicity against human HuH7 cells assessed as cell viability after 48 hrs by CellTiter Glo assay
    Cytotoxicity against human HuH7 cells assessed as cell viability after 48 hrs by CellTiter Glo assay
    [PMID: 26771861]
    MCF7 IC50
    27.3 μM
    Compound: (+/-)-C-75
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
    [PMID: 28324785]
    MDA-MB-231 IC50
    43.8 μM
    Compound: (+/-)-C-75
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
    [PMID: 28324785]
    MIA PaCa-2 IC50
    21.8 μM
    Compound: (+/-)-C-75
    Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTT assay
    Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTT assay
    [PMID: 28324785]
    OVCAR-3 IC50
    21.9 μM
    Compound: (+/-)-C-75
    Antiproliferative activity against human OVCAR3 cells after 72 hrs by MTT assay
    Antiproliferative activity against human OVCAR3 cells after 72 hrs by MTT assay
    [PMID: 28324785]
    PC-3 IC50
    26.8 μM
    Compound: (+/-)-C-75
    Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
    [PMID: 28324785]
    SK-BR-3 IC50
    19.8 μM
    Compound: (+/-)-C-75
    Antiproliferative activity against human SKBR3 cells after 72 hrs by MTT assay
    Antiproliferative activity against human SKBR3 cells after 72 hrs by MTT assay
    [PMID: 28324785]
    體外研究
    (In Vitro)

    C75 抑制 PC3 細(xì)胞生長(zhǎng),24 小時(shí)時(shí)的 IC50 為 35 μM。C75 (10-50 μM) 還以濃度依賴性方式減少 LNCaP 球狀體的生長(zhǎng),IC50 為 50 μM[1]。
    (-)- C75 抑制 FAS 活性并對(duì)腫瘤細(xì)胞系具有細(xì)胞毒性作用,而不影響食物消耗。(+)- C75 抑制 CPT1,其給藥產(chǎn)生厭食,表明 CPT1 的中樞抑制對(duì)于 C75 的厭食作用是必不可少的。C75 對(duì)映異構(gòu)體的不同活性可能會(huì)導(dǎo)致開發(fā)潛在的新的癌癥和肥胖特異性藥物[2]。

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

    體內(nèi)研究
    (In Vivo)

    腹腔注射后 10-24 小時(shí),C75 阻斷空腹誘導(dǎo)的弓狀核 (Arc)、下丘腦外側(cè)區(qū) (LHA) 和室旁核 (PVN) 中的 c-Fos 表達(dá)。腹膜內(nèi)注射 30 mg/kg 體重的 C75 后 2 小時(shí)內(nèi)可抑制小鼠攝食 ≥ 95%[3]。由于脂肪酸氧化,C75 處理的 DIO 小鼠體重減輕了 50%,能量產(chǎn)生增加了 32.9%。C75 處理嚙齒動(dòng)物脂肪細(xì)胞和肝細(xì)胞以及人類乳腺癌細(xì)胞可通過增加 CPT-1 活性來增加脂肪酸氧化和 ATP 水平,即使存在升高濃度的丙二酰輔酶 A 也是如此[4]。

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

    分子量

    254.32

    Formula

    C14H22O4

    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    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 6 months
    -20°C 1 month
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    DMSO 中的溶解度 : 100 mg/mL (393.21 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 3.9321 mL 19.6603 mL 39.3205 mL
    5 mM 0.7864 mL 3.9321 mL 7.8641 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, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(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 (9.83 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。

      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 (9.83 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。

      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

    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: 99.91%

    參考文獻(xiàn)
    Cell Assay
    [1]

    Cells are seeded in 96-well plates and incubated for 2 days to allow exponential phase growth. Cells are then ished twice with PBS and treated with C75. After 24 or 48 h incubation, MTT is added to a final concentration of 0.5 mg/ml and cultures are incubated for 2 h. Cells are then solubilized with DMSO before measuring absorbance at 570 nm. Cell growth is also measured, using MTT assay, every 24 h up to 96 h[1].

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

    Animal Administration
    [3]

    Mice: C75 is administered either by i.p. (i.p.; 30 mg/kg of body weight) or i.c.v. (10 μg in 3 μL of RPMI medium 1640) injection. One, 11.5, and 24 h after i.p. injection, cumulative food intake is measured, mice are killed, brains are sectioned, and slices are subjected to immunohistochemical staining for c-Fos. All i.p. injections are given 1 h before the start of the dark cycle. For i.c.v. injection, mice are anesthetized with metofane and given 3 μl of RPMI medium 1640 (control) or C75 in RPMI medium 1640 into the lateral ventricle with a calibrated 10-μl Hamilton syringe[3].

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

    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, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(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 3.9321 mL 19.6603 mL 39.3205 mL 98.3013 mL
    5 mM 0.7864 mL 3.9321 mL 7.8641 mL 19.6603 mL
    10 mM 0.3932 mL 1.9660 mL 3.9321 mL 9.8301 mL
    15 mM 0.2621 mL 1.3107 mL 2.6214 mL 6.5534 mL
    20 mM 0.1966 mL 0.9830 mL 1.9660 mL 4.9151 mL
    25 mM 0.1573 mL 0.7864 mL 1.5728 mL 3.9321 mL
    30 mM 0.1311 mL 0.6553 mL 1.3107 mL 3.2767 mL
    40 mM 0.0983 mL 0.4915 mL 0.9830 mL 2.4575 mL
    50 mM 0.0786 mL 0.3932 mL 0.7864 mL 1.9660 mL
    60 mM 0.0655 mL 0.3277 mL 0.6553 mL 1.6384 mL
    80 mM 0.0492 mL 0.2458 mL 0.4915 mL 1.2288 mL
    100 mM 0.0393 mL 0.1966 mL 0.3932 mL 0.9830 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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    Inquiry Information

    產(chǎn)品名稱:
    C75
    目錄號(hào):
    HY-12364
    需求量: