2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. A 922500

A 922500  (Synonyms: DGAT-1 Inhibitor 4a)

目录号: HY-10038 纯度: 99.33%
COA 产品使用指南

摩尔计算器

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。

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A 922500 Chemical Structure

A 922500 Chemical Structure

CAS No. : 959122-11-3

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1215
In-stock
1 mg ￥480
In-stock
5 mg ￥1105
In-stock
10 mg ￥1548
In-stock
50 mg ￥4938
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

A 922500 相关抗体

Top Publications Citing Use of Products

    A 922500 purchased from MCE. Usage Cited in: Cell Metab. 2020 Aug 4;32(2):229-242.e8.  [Abstract]

    Effects of Butyrate (But, 1 mM), Valproate (Vpa, 5 mM) and Vorinostat (Vor, 1 μM) on the expression of P-gp and BCRP, NF-кB p65 and phosphorylated p65 (p-p65), and IкBα and phosphorylated IкBα (p-IкBα).

    A 922500 purchased from MCE. Usage Cited in: Cell Metab. 2020 Aug 4;32(2):229-242.e8.  [Abstract]

    Representative fluorescence imaging and quantification of ROS in U251 cells treated with DGAT1 inhibitor A-922500 (20 mg/mL) for 24 h or shRNA for 48 h in the presence or absence of the CPT1 inhibitor Etomoxir (ETO, 6 mM).

    A 922500 purchased from MCE. Usage Cited in: Nat Commun. 2020 Jun 11;11(1):2967.  [Abstract]

    The spatiotemporal distribution of LD is analyzed 5 dpi by immunofluorescence. Compared to DMSO control, cells treated with A922500 (DGAT1i) harbor only scarce LDs. Both the number and average volume of LDs are significantly reduced in the presence of DGAT1i.

    查看 Acyltransferase 亚型特异性产品:

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    ACAT1 ACAT2 MGAT2 ACAT

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    A 922500 (DGAT-1 Inhibitor 4a) is a potent, selective, and orally bioavailable diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of 9 and 22 nM against human and mouse DGAT-1, respectively.

    IC50 & Target

    IC50: 9 nM (human DGAT-1), 22 nM (mouse DGAT-1)[1]
    体外研究
    (In Vitro)

    A 922500 (A-922500) demonstrates excellent selectivity over other acyltransferases, including DGAT-2 (IC50=53 μM) and the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 (IC50=296 μM) [1].

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

    A 922500 相关抗体:
    体内研究
    (In Vivo)

    DGAT-1 inhibitor A 922500 (A-922500) reduces serum triglyceride levels from baseline at all doses tested; however, this is only statistically significant at the 3 mg/kg dose, which lowers serum triglycerides by 53%. Similarly, the 3 mg/kg dose of A 922500 significantly reduces serum FFA concentrations by 55% and total cholesterol by 25%. DGAT-1 inhibition has no significant effect on body weight at any dose tested. Although A 922500 dpes not significantly affect LDL-cholesterol or HDL-cholesterol individually, the serum LDL/HDL-cholesterol ratio is significantly improved by A 922500 at 0.3 and 3 mg/kg. Similar to the dyslipidemic hamster, treatment with 3 mg/kg A 922500 significantly reduces serum triglyceride concentrations (39%). FFA levels significantly increase over the 14-day period in vehicle-treated animals. This increase is inhibited in a dose-dependent manner by A 922500 such that FFA concentrations are 32% lower after 14 days of treatment with the DGAT-1 inhibitor at 3 mg/kg, compared with the vehicle group (p < 0.05). HDL-cholesterol is significantly increased from baseline levels by A 922500 at 0.3 and 3 mg/kg; however, this is only significantly increased compared with vehicle at the 3 mg/kg dose. Body weight significantly increases over the 2-week period in vehicle-treated rats, and this is not affected by A 922500. LDL-cholesterol is significantly reduced in the vehicle treated group. DGAT-1 inhibition does not further reduce LDL-cholesterol and has no effect on total cholesterol[1].

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

    428.48

    Formula

    C26H24N2O4
    CAS 号
    性状

    固体

    颜色

    Off-white to yellow

    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 : ≥ 50 mg/mL (116.69 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.3338 mL 11.6692 mL 23.3383 mL
    5 mM 0.4668 mL 2.3338 mL 4.6677 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)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    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 (5.83 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。

    以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 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： 50% PEG300    50% Saline

      Solubility: 6.67 mg/mL (15.57 mM); 悬浊液; 超声助溶

    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

    g

    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: 99.33%

    COA (284 KB) HNMR (146 KB) RP-HPLC (167 KB) LCMS (380 KB)

    产品使用指南 (1538 KB)
    参考文献
    Animal Administration
    [1]

    Mice and Hamsters[1]
    Thirteen-week-old male Golden Syrian hamsters (n=40), initially weighing approximately 140 g, are used. Ten-week-old Male Zucker fatty rats (n=32), weighing between 270 and 330 g, are used. After collection of baseline lipid profiles, hyperlipidemic hamsters (n=10/group) and Zucker fatty rats (n=8/group) are administered vehicle [20:80 (v/v), polyethylene glycol/hydroxypropyl-β-cyclodextrin (10% w/v)] or DGAT-1 inhibitor A 922500 (A-922500) at 0.03, 0.3, and 3 mg/kg, once daily by oral gavage. The dosing volume is 5 mL/kg. Serum lipid profiles are then measured 3 h after the dose on day 7 and day 14. Hamsters continue to be fed a high-fat diet with 10% fructose in the drinking water throughout the treatment period. Zucker fatty rats remain on standard rodent diet throughout the study.

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

    A 922500 相关分类

    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。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3338 mL 11.6692 mL 23.3383 mL 58.3458 mL
    5 mM 0.4668 mL 2.3338 mL 4.6677 mL 11.6692 mL
    10 mM 0.2334 mL 1.1669 mL 2.3338 mL 5.8346 mL
    15 mM 0.1556 mL 0.7779 mL 1.5559 mL 3.8897 mL
    20 mM 0.1167 mL 0.5835 mL 1.1669 mL 2.9173 mL
    25 mM 0.0934 mL 0.4668 mL 0.9335 mL 2.3338 mL
    30 mM 0.0778 mL 0.3890 mL 0.7779 mL 1.9449 mL
    40 mM 0.0583 mL 0.2917 mL 0.5835 mL 1.4586 mL
    50 mM 0.0467 mL 0.2334 mL 0.4668 mL 1.1669 mL
    60 mM 0.0389 mL 0.1945 mL 0.3890 mL 0.9724 mL
    80 mM 0.0292 mL 0.1459 mL 0.2917 mL 0.7293 mL
    100 mM 0.0233 mL 0.1167 mL 0.2334 mL 0.5835 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.

    Keywords:

    A 922500959122-11-3DGAT-1 Inhibitor 4aA922500A-922500AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseInhibitorinhibitorinhibit

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    目录号：
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