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BMS309403 FABP4 Inhibitor

Cat.No.S6622

BMS309403 is a small-molecule FABP4 inhibitor with nM affinity (Kd=4 nM for FABP4) and >100-fold selectivity against FABP5 as well as the heart isoform FABP3.
BMS309403 FABP inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 474.55

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Quality Control

Batch: Purity: 99.94%
99.94

Cell Culture, Treatment & Working Concentration

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
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Solubility

In vitro
Batch:

DMSO : 95 mg/mL (200.18 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 18 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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%
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% ddH2O
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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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

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

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

Mechanism of Action

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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