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  3. T-5224

T-5224 

製品番号: HY-12270 純度: 99.06%
COA 取扱説明書

T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription.

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T-5224 構造式

T-5224 構造式

CAS 番号 : 530141-72-1

容量 価格(税別) 在庫状況 数量
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 137 在庫あり
Solution
10 mM * 1 mL in DMSO USD 137 在庫あり
Solid
5 mg USD 120 在庫あり
10 mg USD 180 在庫あり
50 mg USD 540 在庫あり
100 mg USD 888 在庫あり
200 mg   お問い合わせ  
500 mg   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

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 48 publication(s) in Google Scholar

Top Publications Citing Use of Products

顧客検証

WB

    T-5224 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Sep;155:275-287.  [Abstract]

    Twist1, nuclear NF-κB-p65 and secreted TNF-α in macrophages after transfection with Twist1 siRNA (100 pmol/well) for 48 h and then treatment with LPS, TT-TFM (200 μM) and T5224 (50 μM) for another 24 h.

    T-5224 purchased from MedChemExpress. Usage Cited in: Endocrinology. 2017 Nov 1;158(11):4064-4075.  [Abstract]

    Cyp27b1 induction by LPS or TNF-α is mediated by NF-κB. HCT116 cells are treated with 100 ng/mL LPS or 100 ng/mL TNF-α overnight in the presence or absence of 20 ng/mL T-5224 as indicated. Cyp27b1 protein levels are measured by Western blotting.
    • 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

    T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription[1][2].

    IC50 & Target

    c-Fos/activator protein (AP)-1[1]

    体外実験

    T-5224 inhibits in-vitro production of the mediators MMP-1, MMP-3, IL-6 and TNF-α by IL-1β-stimulated human synovial SW982 cells with the mean IC50 of about 10 μM[2].
    T-5224 (0-80 μM) significantly inhibits the invasion, migration, and MMP activity of HSC-3-M3 cells in a dose-dependent manner[3].

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

    体内実験

    Administration of T-5224 (300 mg/kg, p.o.) after intraperitoneal injection of LPS impartes appreciable protection against acute elevations in serum levels of TNFα, HMGB1, ALT/AST as well as in liver tissue levels of MIP-1α and MCP-1, and reduces the lethality (27%)[4].
    G2 is observed in rat and monkey liver microsomes as a major metabolite of T-5224, suggesting that G2 is not a human-specific metabolite[5].
    T-5224 (300 mg/kg, p.o.) inhibits the production of TNF-alpha and other downstream effectors in C57BL/6 mice[6].

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

    分子量

    517.53

    分子式

    C29H27NO8

    CAS 番号
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    OC1=NOC2=CC(COC3=C(CCC(O)=O)C=C(C(C4=C(O)C=C(OC5CCCC5)C=C4)=O)C=C3)=CC=C21

    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 : 100 mg/mL (193.23 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9323 mL 9.6613 mL 19.3225 mL
    5 mM 0.3865 mL 1.9323 mL 3.8645 mL
    10 mM 0.1932 mL 0.9661 mL 1.9323 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: 5 mg/mL (9.66 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: 5 mg/mL (9.66 mM); Clear solution; Need ultrasonic

    *All of the co-solvents are available by MedChemExpress (MCE).
    純度とドキュメンテーション

    純度: 99.59%

    参考文献
    細胞実験
    [4]

    HSC-3-M3 cells are starved for 24 h with DMEM containing 0.5% FBS. The top chamber of the cell invasion device is coated with 50 μL of 0.1 × basement membrane extract solution and incubataed overnight. HSC-3-M3 cells (5.0 × 104 cells/well) are added to the top chamber with DMEM containing 0.5% FBS mixed with 0-80 μM T-5224; DMEM with 10% FBS is added to the bottom chamber and incubated for 48 h. The bottom plate is read using a multilabel plate reader. The data are compared with the standard curve to determine the fraction of invaded cells.

    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。

    動物実験
    [2]

    Mice in LPS group are administered orally with polyvinylpyrrolidone solution in the same volume of T-5224 solution immediately after LPS injection, while in the T-5224 group, mice are administered orally with T-5224 (300 mg/kg, p.o.) in the same manner. In the control group, mice receives polyvinylpyrrolidone solution orally soon after intraperitoneal saline injection. Blood samples are collected for each measurement at the optimal time.

    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
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    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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    製品名:
    T-5224
    製品番号:
    HY-12270
    数量:
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