2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. FABP Interleukin Related
  4. FABP4/5-IN-6

FABP4/5-IN-6 is an orally active, potent FABP4/5 inhibitor (Ki = 0.41/2.53 μM), showing low selectivity over FABP3 (Ki = 59.72 μM). FABP4/5-IN-6 inhibits the secretion of MCP-1 and IL-6 in Lipopolysaccharides (HY-D1056) (LPS)-induced THP-1 macrophage. FABP4/5-IN-6 exhibits significant anti-inflammatory effects and attenuates LPS-induced liver injury. FABP4/5-IN-6 has low hERG inhibition (LD50 > 2000 mg/kg). FABP4/5-IN-6 can be used for the study of Inflammation-related diseases.

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FABP4/5-IN-6

FABP4/5-IN-6 Chemical Structure

CAS No. : 2975215-64-4

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FABP4/5-IN-6 Related Antibodies

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Description

FABP4/5-IN-6 is an orally active, potent FABP4/5 inhibitor (Ki = 0.41/2.53 μM), showing low selectivity over FABP3 (Ki = 59.72 μM). FABP4/5-IN-6 inhibits the secretion of MCP-1 and IL-6 in Lipopolysaccharides (HY-D1056) (LPS)-induced THP-1 macrophage. FABP4/5-IN-6 exhibits significant anti-inflammatory effects and attenuates LPS-induced liver injury. FABP4/5-IN-6 has low hERG inhibition (LD50 > 2000 mg/kg). FABP4/5-IN-6 can be used for the study of Inflammation-related diseases[1].

In Vitro

FABP4/5-IN-6 (Compound Y18) (80 μM, 24 h) shows no significant cytotoxicity to THP-1 cells, and cell viability is unaffected[1].
FABP4/5-IN-6 (5-25 μM, 24 h) significantly inhibits LPS-induced secretion of MCP-1 and IL-6 in THP-1 macrophage cells, with the inhibitory effect showing a dose-dependent effect[1].

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

FABP4/5-IN-6 Related Antibodies

ELISA Assay[1]

Cell Line: LPS-induced THP-1 macrophage cells
Concentration: 5 μM, 10 μM, 25 μM
Incubation Time: Incubate 18 hours, then stimulate with LPS (100 ng/mL) for 6 hours
Result: Significantly reduced the secretion of MCP-1 and IL-6.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-24 MRT F CL Vss
Mice 25 mg/kg p.o. 3.22 h 0.33 h 32.94 μg/mL 88.87 μg·h/mL 4.33 h 32 % / /
Mice 3 mg/kg i.v. 4.17 h / / 33.3 μg·h/mL 3.64 h / 1.48 mL/mg/kg 0.324 L/kg
In Vivo

FABP4/5-IN-6 (Compound Y18) (50 mg/kg, p.o., once daily for 4 days) exhibits significant anti-inflammatory and protective effects in mice. It effectively reduces LPS-induced liver damage, inhibits systemic and local hepatic inflammatory responses, and improves pathological damage to the liver and spleen[1].

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

Animal Model: Seven-week-old male C57BL/6 mice were used to develop an acute inflammation model induced by LPS[1].
Dosage: 50 mg/kg
Administration: P.o., once daily for 4 days, LPS was injected 30 minutes after the last dose
Result: Body weight remained unchanged.
Significantly reduced serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels.
Significantly inhibited LPS-induced MCP-1 elevation.
Exhibited a trend toward reducing serum IL-6 and TNF-α levels.
Reduced inflammatory cell infiltration and alleviated pathological changes in the spleen.
Significantly inhibited the LPS-induced upregulation of liver MCP-1 and CD11b (macrophage marker) gene expression, and showed an inhibitory trend on IL-6 and TNF-α gene expression.
Molecular Weight

420.26

Formula

C21H16Cl2FNO3
CAS No.
SMILES

O=C1C2=CC=C(C=C2C(C3=CC=C(C(Cl)=C3)F)=C(N1C4CCCC4)C(O)=O)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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FABP4/5-IN-6 Related Classifications

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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.

Keywords:

FABP4/5-IN-62975215-64-4FABPInterleukin RelatedFatty acid-binding proteinILFABP4FABP5Anti-InflammatoryLPS-Induced Liver InjuryInhibitorinhibitorinhibit

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