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

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

製品番号: HY-10038 純度: 99.33%
COA 取扱説明書 Technical Support

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.

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CAS 番号 : 959122-11-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 138 在庫あり
Solution
10 mM * 1 mL in DMSO USD 138 在庫あり
Solid
1 mg $56 在庫あり
5 mg $126 在庫あり
10 mg $176 在庫あり
25 mg $346 在庫あり
50 mg $485 在庫あり
100 mg $680 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 30 publication(s) in Google Scholar

Other Forms of A 922500:

A 922500 関連抗体

Top Publications Citing Use of Products

顧客検証

WB
IF

    A 922500 purchased from MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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.

    Acyltransferase アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    ACAT1 ACAT2 MGAT2 ACAT DGAT1 DGAT2

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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]
    Cellular Effect
    Cell Line Type Value Description References
    Sf9 IC50
    20 1
    Compound: 4
    Inhibition of human DGAT1 expressed in Sf9 cells assessed as formation of didecanoylglycerol product after 1 hr using 14C-decanoyl-CoA by beta scintillation counter
    Inhibition of human DGAT1 expressed in Sf9 cells assessed as formation of didecanoylglycerol product after 1 hr using 14C-decanoyl-CoA by beta scintillation counter
    		[PMID: 21868220]
    Sf9 IC50
    20 1
    Compound: 4
    Inhibition of human DGAT1 expressed in Sf9 cells assessed as formation of didecanoylglycerol product after 1 hr using 14C-decanoyl-CoA by beta scintillation counter
    Inhibition of human DGAT1 expressed in Sf9 cells assessed as formation of didecanoylglycerol product after 1 hr using 14C-decanoyl-CoA by beta scintillation counter
    		[PMID: 21868220]
    Sf9 IC50
    0.007 3
    Compound: 4a
    Inhibition of human recombinant DGAT1 expressed in Sf9 cells
    Inhibition of human recombinant DGAT1 expressed in Sf9 cells
    		[PMID: 18183944]
    Sf9 IC50
    0.007 3
    Compound: 4a
    Inhibition of human recombinant DGAT1 expressed in Sf9 cells
    Inhibition of human recombinant DGAT1 expressed in Sf9 cells
    		[PMID: 18183944]
    Sf9 IC50
    0.024 3
    Compound: 4a
    Inhibition of mouse recombinant DGAT1 expressed in Sf9 cells
    Inhibition of mouse recombinant DGAT1 expressed in Sf9 cells
    		[PMID: 18183944]
    Sf9 IC50
    0.024 3
    Compound: 4a
    Inhibition of mouse recombinant DGAT1 expressed in Sf9 cells
    Inhibition of mouse recombinant DGAT1 expressed in Sf9 cells
    		[PMID: 18183944]
    Sf9 IC50
    20 1
    Compound: 4
    Inhibition of human DGAT1 expressed in Sf9 cells assessed as formation of didecanoylglycerol product after 1 hr using 14C-decanoyl-CoA by beta scintillation counter
    Inhibition of human DGAT1 expressed in Sf9 cells assessed as formation of didecanoylglycerol product after 1 hr using 14C-decanoyl-CoA by beta scintillation counter
    		[PMID: 21868220]
    体外実験

    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].

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

    A 922500 関連抗体
    体内実験

    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].

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

    428.48

    分子式

    C26H24N2O4
    CAS 番号
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    O=C(NC1=CC=C(C2=CC=C(C([C@@H]3CCC[C@H]3C(O)=O)=O)C=C2)C=C1)NC4=CC=CC=C4
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 50 mg/mL (116.69 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.2334 mL 1.1669 mL 2.3338 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 6.67 mg/mL (15.57 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.33%

    COA (247 KB) HNMR (146 KB) RP-HPLC (167 KB) LCMS (379 KB)

    取扱説明書 (2659 KB)
    参考文献
    動物実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 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
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    A 922500 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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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    製品名:
    A 922500
    製品番号:
    HY-10038
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