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.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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.
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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.
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
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.
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (237.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3795 mL | 11.8974 mL | 23.7948 mL | 59.4870 mL |
| 5 mM | 0.4759 mL | 2.3795 mL | 4.7590 mL | 11.8974 mL | |
| 10 mM | 0.2379 mL | 1.1897 mL | 2.3795 mL | 5.9487 mL | |
| 15 mM | 0.1586 mL | 0.7932 mL | 1.5863 mL | 3.9658 mL | |
| 20 mM | 0.1190 mL | 0.5949 mL | 1.1897 mL | 2.9743 mL | |
| 25 mM | 0.0952 mL | 0.4759 mL | 0.9518 mL | 2.3795 mL | |
| 30 mM | 0.0793 mL | 0.3966 mL | 0.7932 mL | 1.9829 mL | |
| 40 mM | 0.0595 mL | 0.2974 mL | 0.5949 mL | 1.4872 mL | |
| 50 mM | 0.0476 mL | 0.2379 mL | 0.4759 mL | 1.1897 mL | |
| 60 mM | 0.0397 mL | 0.1983 mL | 0.3966 mL | 0.9914 mL | |
| 80 mM | 0.0297 mL | 0.1487 mL | 0.2974 mL | 0.7436 mL | |
| 100 mM | 0.0238 mL | 0.1190 mL | 0.2379 mL | 0.5949 mL |
FABP4/5-IN-6 Related Classifications
HY-178471 Related Classifications
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