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Cat.No.S6622
| Related Targets | Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism |
|---|---|
| Other FABP Products | FABP4 Antibody [M24L23] FABP5 Antibody [D10L18] FABP7 Antibody [B3J10] |
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| BL21(DE3) | Function assay | Displacement of 1,8-ANS from His6-tagged FABP4 (unknown origin) expressed in Escherichia coli BL21(DE3) cells by fluorescence assay, Ki=0.22μM | 27460668 | |||
| BL21(DE3) | Function assay | Direct binding to His6-tagged FABP4 (unknown origin) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry, Kd=2.05μM | 27460668 | |||
| aP2+/+ macrophage cells | Function assay | 24 hrs | Decrease in MCP1 production in mouse aP2+/+ macrophage cells after 24 hrs | 17554340 | ||
| aP2-/-R macrophage cells | Function assay | 24 hrs | Decrease in MCP1 production in mouse aP2-/-R macrophage cells (re-expression of aP2) after 24 hrs | 17554340 | ||
| THP1 | Function assay | 25 uM | 3 days | Reduction of transformation of human THP1 cells to foam cells at 25 uM after 3 days relative to control | 17554340 | |
| aP2+/+ macrophage cells | Function assay | 25 uM | Reduction in total cholesterol ester content in mouse aP2+/+ macrophage cells at 25 uM relative to control | 17554340 | ||
| aP2-/-R macrophage cells | Function assay | 25 uM | Reduction in total cholesterol ester content in mouse aP2-/-R macrophage cells (re-expression of aP2) at 25 uM relative to control | 17554340 | ||
| THP1 | Function assay | 25 uM | Increase in APOA1-mediated cholesterol in human THP1 cells at 25 uM relative to control | 17554340 | ||
| THP1 | Function assay | 25 uM | Increase in ABCA1 mRNA level in human THP1 cells at 25 uM relative to control | 17554340 | ||
| THP1 | Function assay | 25 uM | Increase in ABCA1 protein level in human THP1 cells at 25 uM relative to control | 17554340 | ||
| aP2+/+ macrophage cells | Function assay | 25 uM | Increase in cholesterol efflux in mouse aP2+/+ macrophage cells at 25 uM relative to control | 17554340 | ||
| aP2-/-R macrophage cells | Function assay | 25 uM | Increase in cholesterol efflux in mouse aP2-/-R macrophage cells (re-expression of aP2) at 25 uM relative to control | 17554340 | ||
| THP1 | Function assay | Reduction of Mcp1 expression in human THP1 cells expressing aP2 relative to control | 17554340 | |||
| aP2+/+ macrophage cells | Function assay | Reduction of Mcp1 expression mouse aP2+/+ macrophage cells relative to control | 17554340 | |||
| aP2-/-R macrophage cells | Function assay | Reduction of Mcp1 expression mouse aP2-/-R macrophage cells (re-expression of aP2) relative to control | 17554340 | |||
| THP1 | Function assay | Reduction of IL1-beta expression in human THP1 cells expressing aP2 relative to control | 17554340 | |||
| aP2+/+ macrophage cells | Function assay | Reduction of IL1-beta expressed in mouse aP2+/+ macrophage cells relative to control | 17554340 | |||
| aP2-/-R macrophage cells | Function assay | Reduction of IL1-beta expressed in mouse aP2-/-R macrophage cells (re-expression of aP2) relative to control | 17554340 | |||
| THP1 | Function assay | Reduction of IL6 expression in human THP1 cells expressing aP2 relative to control | 17554340 | |||
| aP2+/+ macrophage cells | Function assay | Reduction of IL6 expression mouse aP2+/+ macrophage cells relative to control | 17554340 | |||
| aP2-/-R macrophage cells | Function assay | Reduction of IL6 expression mouse aP2-/-R macrophage cells (re-expression of aP2) relative to control | 17554340 | |||
| THP1 | Function assay | Reduction of TNF expression in human THP1 cells expressing aP2 relative to control | 17554340 | |||
| aP2+/+ macrophage cells | Function assay | Reduction of TNF expression in mouse aP2+/+ macrophage cells relative to control | 17554340 | |||
| aP2-/-R macrophage cells | Function assay | Reduction of TNF expression mouse aP2-/-R macrophage cells (re-expression of aP2) relative to control | 17554340 | |||
| Click to View More Cell Line Experimental Data | ||||||
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In vitro |
DMSO
: 95 mg/mL
(200.18 mM)
Ethanol : 18 mg/mL Water : Insoluble |
|
In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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| Molecular Weight | 474.55 | Formula | C31H26N2O3 |
Storage (From the date of receipt) | 3 years -20°C powder |
|---|---|---|---|---|---|
| CAS No. | 300657-03-8 | -- | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | CCC1=C(C(=NN1C2=CC=CC=C2C3=CC(=CC=C3)OCC(=O)O)C4=CC=CC=C4)C5=CC=CC=C5 | ||
| Targets/IC50/Ki |
FABP4
(Cell-free assay) 4 nM(Kd)
|
|---|---|
| In vitro |
Treatment of BMS309403 (FABP4 inhibitor) comobined with SSO (CD36 inhibitor) significantly decreases the breast cancer cell viability, proliferative, migratory, and invasive abilities over 72 h. Inhibiting either at recommended concentrations does not significantly decrease the breast cancer cell viability over 72 h. Treatment with both SSO and this compound results in clustering of cells and increased lipid content, indicating an inability to metabolise lipids resulting potentially in lipotoxicity-induced apoptosis. |
| In vivo |
Treatment with either BMS309403 or SSO alone decreases the rate of tumour formation and the combination of this compound and SSO significantly decreased the rate of tumour formation. |
References |
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