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.
For research use only. We do not sell to patients.
- CAS No.: 2975215-64-4
- Formula: C21H16Cl2FNO3
- Molecular Weight:420.26
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
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Cell Line:LPS-induced THP-1 macrophage cells
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Concentration:5 μM, 10 μM, 25 μM
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Incubation Time:Incubate 18 hours, then stimulate with LPS (100 ng/mL) for 6 hours
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Result:Significantly reduced the secretion of MCP-1 and IL-6.
| 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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Seven-week-old male C57BL/6 mice were used to develop an acute inflammation model induced by LPS[1].
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Dosage:50 mg/kg
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Administration:P.o., once daily for 4 days, LPS was injected 30 minutes after the last dose
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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.
Chemical Information
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CAS No. 2975215-64-4
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Molecular Weight 420.26
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Formula C21H16Cl2FNO3
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SMILES
O=C1C2=CC=C(C=C2C(C3=CC=C(C(Cl)=C3)F)=C(N1C4CCCC4)C(O)=O)Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FABP4/5-IN-6 Related Classifications
HY-178471 Related Classifications
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