FHND5032
Based on 1 Customer Validation
FHND5032 is an orally active miR-124 inducer. FHND5032 significantly upregulates miR-124 expression in macrophages. FHND5032 disrupts inflammatory signaling, promotes macrophage reprogramming, and restores the epithelial barrier function by inhibiting the PIK3R2/PI3K/Akt axis. FHND5032 alleviates colitis and reduces inflammatory burden in ulcerative colitis mice. FHND5032 can be used for the study of ulcerative colitis.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.92%
- CAS. Nr.: 3076057-63-8
- Formel: C15H9ClF3N3O
- Molecular Weight:339.70
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
In Vitro
FHND5032 (0-20 μM, 24 h) significantly exerts anti-inflammatory activity in THP-1 and RAW 264.7 cells by enhancing miR-124 expression[1]. FHND5032 (≤ 5 μM) activates miR-124-5p expression to regulate the PI3K/Akt pathway by targeting PIK3R2 in THP-1 and RAW 264.7 cells reprogramming[1]. FHND5032 decreases the expression of M1 marker CD86 while increasing the expression of M2 marker CD206 in RAW 264.7 cells[1]. FHND5032 promots the expression of the barrier-sealing proteins ZO-1 and occludin to facilitate Tight junction (TJ) assembly in Caco-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 and RAW 264.7 cells
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Concentration:5, 10 μM
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Incubation Time:/
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Result:Upregulated miR-124 levels and induced miR-124 expression, which peaked at a concentration of 5 μM. Decreased TNF-α, IL-1β, and IL-6 expression in LPS (HY-D1056)- and IFN-γ-stimulated THP-1 cells and LPS stimulated RAW 264.7 cells. Decreased the expression of PIK3R2
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DSS-induced female C57BL/6J mice (18-20 g)[1]
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Dosage:25, 50 mg/kg
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Administration:i.g. once daily for 12 days
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Result:Restrained the body weight loss of DSS-induced colitis mice. Reduced the hematochezia occurrence during treatment. Showed longer colon length of mice. Protected the colonic barrier from pathological damage. Decreased the local level of UC-associated myeloperoxidase (MPO) in the colon. Reduced the expression of pro-inflammatory cytokines, including IL-6, TNF-α, and IFN-γ. Increased the expression of anti-inflammatory cytokines IL-10. Prevented intestinal damage in UC through elevation of TJ proteins. Prevented the FITC-dextran leakage. Inhibited colonic inflammation and repaired the intestinal barrier in colitis mice. Upregulated the miR-124 expression and decreased PIK3R2 expression. Attenuated PIK3R2 upregulation and the hyperphosphorylation of PI3K and Akt. Showed no significant discrepancies in serum physicochemical parameters (alanine aminotransferase (ALT), aspartate aminotransferase (AST), blood urea nitrogen (BUN), and creatinine (Cr)). Decreased the abundance of Proteobacteria in colitis mice and effectively enhanced the relative abundance of Firmicutes. Showed no increase on the abundance of Bacteroidota.
Chemical Information
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CAS. Nr. 3076057-63-8
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Appearance Solid
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Molecular Weight 339.70
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Formel C15H9ClF3N3O
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Color Light yellow to yellow
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SMILES
FC(F)(OC1=CC=C(C=C1)NC2=NC3=CC(Cl)=CC=C3C=N2)F
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 50 mg/mL (147.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 5 mg/mL (14.72 mM); Suspended solution
This protocol yields a suspended solution of ≥ 5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.9438 mL | 14.7189 mL | 29.4377 mL | 73.5943 mL |
| 5 mM | 0.5888 mL | 2.9438 mL | 5.8875 mL | 14.7189 mL | |
| 10 mM | 0.2944 mL | 1.4719 mL | 2.9438 mL | 7.3594 mL | |
| 15 mM | 0.1963 mL | 0.9813 mL | 1.9625 mL | 4.9063 mL | |
| 20 mM | 0.1472 mL | 0.7359 mL | 1.4719 mL | 3.6797 mL | |
| 25 mM | 0.1178 mL | 0.5888 mL | 1.1775 mL | 2.9438 mL | |
| 30 mM | 0.0981 mL | 0.4906 mL | 0.9813 mL | 2.4531 mL | |
| 40 mM | 0.0736 mL | 0.3680 mL | 0.7359 mL | 1.8399 mL | |
| 50 mM | 0.0589 mL | 0.2944 mL | 0.5888 mL | 1.4719 mL | |
| 60 mM | 0.0491 mL | 0.2453 mL | 0.4906 mL | 1.2266 mL | |
| 80 mM | 0.0368 mL | 0.1840 mL | 0.3680 mL | 0.9199 mL | |
| 100 mM | 0.0294 mL | 0.1472 mL | 0.2944 mL | 0.7359 mL |
FHND5032 Related Classifications
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