2. Metabolic Enzyme/Protease
  3. FABP
  4. BMS-309403

BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.

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CAS 番号 : 300657-03-8

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 64 在庫あり
Solution
10 mM * 1 mL in DMSO USD 64 在庫あり
Solid
5 mg $61 在庫あり
10 mg $110 在庫あり
25 mg $220 在庫あり
50 mg $350 在庫あり
100 mg $530 在庫あり
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カスタマーレビュー

Based on 25 publication(s) in Google Scholar

Other Forms of BMS-309403:

BMS-309403 関連抗体

Top Publications Citing Use of Products

    BMS-309403 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2023 Oct 28:575:216403.  [Abstract]

    STAM mice were treated with small-molecule inhibitors targeting LPL (Orlistat, S+O), FABP4 (BMS309403 (15 mg/kg, ip, twice a week), S+B), or CPT1 (Etomoxir, S+E). Tumor burden was reduced in all inhibitor-treated groups compared to the STAM control group.

    BMS-309403 purchased from MedChemExpress. Usage Cited in: Bone Res. 2022 Jun 22;10(1):45.  [Abstract]

    The effect of FABP4 and M1-polarized macrophage supernatant on HUVECs, FLSs, and chondrocytes in vitro. Tube formation assay and quantification of HUVECs cultured with vehicle (C), rhFABP4 (P), rhFABP4 + BMS309403 (20 μmol/L, 1h) (PB). Scale bar: 100 µm.

    BMS-309403 purchased from MedChemExpress. Usage Cited in: Bone Res. 2022 Jun 22;10(1):45.  [Abstract]

    The effect of FABP4 and M1-polarized macrophage supernatant on HUVECs, FLSs, and chondrocytes in vitro. Tube formation assay and quantification of HUVECs cultured with vehicle (C), M1-polarized macrophage supernatant (S), or M1-polarized macrophage supernatant+BMS309403 (20 μmol/L, 1h) (SB) (n = 3 per group). Scale bar: 100 µm.

    BMS-309403 purchased from MedChemExpress. Usage Cited in: Bone Res. 2022 Jun 22;10(1):45.  [Abstract]

    Representative images and quantification of FABP4 immunohistochemical staining and coimmunostaining of FABP4 with F4/80 or NOS2 in the synovium of TSC1KO mice treated with vehicle, BMS309403 (5 mg/kg, ip, twice a week) or anagliptin for 4 weeks after AIA modeling (n = 10 per group). Scale bar: 12.5 µm and 100 µm.

    BMS-309403 purchased from MedChemExpress. Usage Cited in: Bone Res. 2022 Jun 22;10(1):45.  [Abstract]

    Representative images and quantification of FABP4 immunohistochemical staining and coimmunostaining of FABP4 with F4/80 or NOS2 in the synovium of TSC1KO mice treated with vehicle, BMS309403 (5 mg/kg, ip, twice a week) or anagliptin for 8 weeks after AIA modeling (n = 10 per group). Scale bar: 12.5 µm and 100 µm.

    BMS-309403 purchased from MedChemExpress. Usage Cited in: Am J Cancer Res. 2019 Oct 1;9(10):2140-2155.  [Abstract]

    FABP4 expression is up-regulated in the metastatic tumor sites. BALB/C nude mice are intrahepatic inoculation of 5 × 106 HepG2 cells followed by intraperitoneally injection with PBS or 25-HC (10 mg/kg) or 25-HC with BMS-309403 (45 mg/kg). At the end of the experiment, mice are sacrificed, the tumor tissues in the livers of the mice without metastasis, with abdominal metastasis and the metastatic tumor sites are extracted. The mRNA and protein expression of FABP4 is assessed by RT-qPCR

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    製品説明

    BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells[1][2][3].

    IC50 & Target

    Ki: less than 2 nM (FABP4), 250 nM (FABP3), 350 nM (FABP5)[1]
    体外実験

    Treatment with BMS-309403 significantly decreased MCP-1 production from THP-1 macrophages in a dose- and time-dependent manner[2].

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

    BMS-309403 関連抗体
    体内実験

    BMS-309403 sodium (15 mg/kg; chronic treatment; daily for 6 weeks) improves endothelial function, phosphorylated and total eNOS and reduced plasma triglyceride levels but did not affect endothelium-independent relaxations[3].

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

    Animal Model: C57BL/6J mice (ApoE−/− mice)[3]
    Dosage: 15 mg/kg
    Administration: Chronic treatment ; daily for 6 weeks
    Result: Significantly increased the phosphorylated eNOS (Ser1177) and total eNOS but not the phosphorylated to total eNOS ratio in aortae of 18 weeks old ApoE−/− mice.
    分子量

    474.55

    分子式

    C31H26N2O3
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)COC1=CC(C2=CC=CC=C2N3N=C(C4=CC=CC=C4)C(C5=CC=CC=C5)=C3CC)=CC=C1
    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 : 175 mg/mL (368.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1073 mL 10.5363 mL 21.0726 mL
    5 mM 0.4215 mL 2.1073 mL 4.2145 mL
    10 mM 0.2107 mL 1.0536 mL 2.1073 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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    一般には略語で表示されます：C1V1 = C2V2

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    純度とドキュメンテーション

    純度: 99.91%

    COA (255 KB) HNMR (296 KB) LCMS (94 KB)

    取扱説明書 (2659 KB)
    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1073 mL 10.5363 mL 21.0726 mL 52.6815 mL
    5 mM 0.4215 mL 2.1073 mL 4.2145 mL 10.5363 mL
    10 mM 0.2107 mL 1.0536 mL 2.1073 mL 5.2681 mL
    15 mM 0.1405 mL 0.7024 mL 1.4048 mL 3.5121 mL
    20 mM 0.1054 mL 0.5268 mL 1.0536 mL 2.6341 mL
    25 mM 0.0843 mL 0.4215 mL 0.8429 mL 2.1073 mL
    30 mM 0.0702 mL 0.3512 mL 0.7024 mL 1.7560 mL
    40 mM 0.0527 mL 0.2634 mL 0.5268 mL 1.3170 mL
    50 mM 0.0421 mL 0.2107 mL 0.4215 mL 1.0536 mL
    60 mM 0.0351 mL 0.1756 mL 0.3512 mL 0.8780 mL
    80 mM 0.0263 mL 0.1317 mL 0.2634 mL 0.6585 mL
    100 mM 0.0211 mL 0.1054 mL 0.2107 mL 0.5268 mL
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    BMS-309403 Related Classifications

    • Molarity Calculator

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    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:

    BMS-309403300657-03-8BMS309403BMS 309403FABPFatty acid-binding proteinglucoseuptakeendothelialfunctionselectiveoralInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
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