1. Metabolic Enzyme/Protease
  2. Acyltransferase
  3. Avasimibe

Avasimibe (Synonyms: CI-1011; PD-148515)

製品番号: HY-13215 純度: 99.58%
取扱説明書

Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively. Avasimibe can be used for the research of prostate cancer.

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Avasimibe 構造式

Avasimibe 構造式

CAS 番号 : 166518-60-1

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
Solution
10 mM * 1 mL in DMSO USD 61 在庫あり
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 61 在庫あり
Estimated Time of Arrival: December 31
Solid
10 mg USD 55 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 198 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 352 在庫あり
Estimated Time of Arrival: December 31
200 mg USD 572 在庫あり
Estimated Time of Arrival: December 31
500 mg   お問い合わせ  
1 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 8 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Avasimibe purchased from MCE. Usage Cited in: Biomed Pharmacother. 2020 Oct;130:110508.

    qRT-PCR data showing the expression of linc00339 in T98 G or LN229 cells treated with linc00339 plasmid, Avasimibe (7.5 μM for 48 h) alone or in combination with linc00339 plasmids.

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

    • 生物活性

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    製品説明

    Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively[1]. Avasimibe can be used for the research of prostate cancer[2].

    IC50 & Target[1]

    ACAT1

    24 μM (IC50)

    ACAT2

    9.2 μM (IC50)

    体外実験

    Avasimibe (0, 0.25, 5, 10, 20, 40 and 80 µM; for 1, 2, and 3 days) reduces proliferation in the prostate cancer (PCa) cells[2].
    Avasimibe (10 and 20 µM; 48 h) reduces the expression of β-catenin, Vimentin, N-cadherin, Snail and MMP9, which are tightly associated with epithelial-mesenchymal transition (EMT)[2].
    Avasimibe (10 and 20 µM) trigger cell cycle arrest via the E2F-1 signalling pathway in prostate cancer. Avasimibe induces G1 phase cell cycle arrest of PCa cells[2].
    Avasimibe (10 and 20 µM) inhibits the metastasis of PCa cells[2].

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

    Cell Viability Assay[2]

    Cell Line: PCa cells (PC-3 and DU 145)
    Concentration: 0, 0.25, 5, 10, 20, 40 and 80 µM
    Incubation Time: 1, 2, and 3 days
    Result: Dose dependently inhibited PC-3 and DU 145 cell viability.

    Western Blot Analysis[2]

    Cell Line: PCa cells (PC-3 and DU 145)
    Concentration: 10 and 20 µM
    Incubation Time: 48 hours
    Result: Reduced protein levels of EMT-related proteins (β-catenin, Vimentin, N-cadherin, Snail, MMP9 and E-cadherin).

    Cell Cycle Analysis[2]

    Cell Line: PCa cells (PC-3 and DU 145)
    Concentration: 10 and 20 µM
    Incubation Time: 48 hours
    Result: Induced G1 phase cycle arrest and altered the G1 phase-related protein levels in PCa cells.
    体内実験

    Avasimibe (30 mg/kg, intraperitoneally injected on alternate days for 7 weeks) suppresses PCa cell growth and metastasis in vivo. Avasimibe has good biocompatibility and low toxicity[2].

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

    Animal Model: SPF male mice (BALB/c-nude, 4 weeks old) bearing PCa cells[2]
    Dosage: 30 mg/kg
    Administration: Intraperitoneally injected for 7 weeks
    Result: Reduced tumour volume compared with that of the control group. Inhibited PCa growth and migration in vivo.
    分子量

    501.72

    分子式

    C29H43NO4S

    CAS 番号
    SMILES

    O=C(NS(=O)(OC1=C(C(C)C)C=CC=C1C(C)C)=O)CC2=C(C(C)C)C=C(C(C)C)C=C2C(C)C

    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 : 250 mg/mL (498.29 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9931 mL 9.9657 mL 19.9314 mL
    5 mM 0.3986 mL 1.9931 mL 3.9863 mL
    10 mM 0.1993 mL 0.9966 mL 1.9931 mL
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 1.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.25 mg/mL (4.48 mM); Suspended solution; Need ultrasonic

    • 2.

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

      Solubility: 2.08 mg/mL (4.15 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (4.15 mM); Clear solution

    *All of the co-solvents are available by MCE.
    参考文献

    純度: 99.58%

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    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
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    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

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    製品名:
    Avasimibe
    製品番号:
    HY-13215
    数量:
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