H052
Based on 1 Customer Validation
H052 is a potent Staphylococcus aureus α-hemolysin (Hla) inhibitor. H052 specifically binds to the W286 residue of the Hla monomer, preventing its oligomerization into a heptameric transmembrane pore, thereby completely blocking calcium ion influx and subsequent cell damage and barrier disruption. H052 can be used for research on pulmonary infections caused by S. aureus.
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- Pureté : 98.18%
- CAS No.: 2886748-00-9
- Formule: C21H15ClFN3O4S
- Masse moléculaire:459.88
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
Hla |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U-937 | EC50 |
10 nM
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Inhibition of Hla-induced Ca2+ influx in human U937 leukocyte cells by Fluo-4 fluorescence assay.
Inhibition of Hla-induced Ca2+ influx in human U937 leukocyte cells by Fluo-4 fluorescence assay.
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40168998 |
| Monocyte | EC50 |
90 nM
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Inhibition of Hla-induced Ca2+ influx in freshly isolated human CD14+ monocytes by fluorescence assay.
Inhibition of Hla-induced Ca2+ influx in freshly isolated human CD14+ monocytes by fluorescence assay.
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40168998 |
In Vitro
H052 (90 nM) inhibits Hla-induced Ca2+ influx in human CD14+ monocytes with EC50 90 nM[1].
H052 (0.04 mM for Hla-induced LDH release; 100 μM for standard cytotoxicity; 72 h) prevents Hla-induced LDH release in A549 cells and is not cytotoxic up to 100 μM[1].
H052 (7.3 mM) protects human airway epithelial cells from Hla-induced cell death in a live-dead assay with EC50 7.3 mM[1].
H052 (4.0 mM) completely protects Calu-3 epithelial barrier integrity from Hla-induced TEER loss at 4.0 mM[1].
H052 (1.6 μM) prevents Hla-induced adherens junction degradation in HPMEC at 1.6 μM[1].
H052 directly binds Hla at W286 to inhibit functional pore formation in biochemical/cell-free assays[2].
H052 protects epithelial and endothelial cells along with erythrocytes and immune cells from Hla-induced damage and covers 79% of published Hla isolates[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:1, 5, 10 μM
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Incubation Time:6 h
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Result:Prevented apoptosis induced by bacterial infection in a dose-dependent manner
Parmacokinetics
| Species | Dose | Route | T1/2 | C0 | AUC0-t | Vz | CL |
|---|---|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 1.67 h | 1448 ng/mL | 2001 ng·h/mL | 1.17 L/kg | 8.2 mL/min/kg |
In Vivo
H052 (60 mg/kg; i.p.; twice daily; 4 days) significantly improves animal survival in the S. aureus intranasal infection pneumonia model in C57BL/6 mice[1].
H052 (60 mg/kg; i.p.; twice daily; from 1 h post-infection to 4 days post-infection or from one day pre-infection to 4 days post-infection) improves survival rate when administered either post-infection or pre-infection in the S. aureus pneumonia model, and enhances the efficacy of Linezolid (HY-10394)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6N (male, 7-8 weeks old)[1]
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Dosage:60 mg/kg
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Administration:i.p.; twice daily; 4 days
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Result:Improved survival compared with vehicle control.
Mice with a high disease score after infection completely recovered over time.
Chemical Information
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CAS No. 2886748-00-9
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Appearance Solid
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Masse moléculaire 459.88
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Formule C21H15ClFN3O4S
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Color White to light brown
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SMILES
O=C1NC2=C(C=C(C)C(S(NC3=CC=C(C4=CC=C(F)C=C4)C(Cl)=C3)(=O)=O)=C2)NC1=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (217.45 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.
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 (5.44 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.44 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1745 mL | 10.8724 mL | 21.7448 mL | 54.3620 mL |
| 5 mM | 0.4349 mL | 2.1745 mL | 4.3490 mL | 10.8724 mL | |
| 10 mM | 0.2174 mL | 1.0872 mL | 2.1745 mL | 5.4362 mL | |
| 15 mM | 0.1450 mL | 0.7248 mL | 1.4497 mL | 3.6241 mL | |
| 20 mM | 0.1087 mL | 0.5436 mL | 1.0872 mL | 2.7181 mL | |
| 25 mM | 0.0870 mL | 0.4349 mL | 0.8698 mL | 2.1745 mL | |
| 30 mM | 0.0725 mL | 0.3624 mL | 0.7248 mL | 1.8121 mL | |
| 40 mM | 0.0544 mL | 0.2718 mL | 0.5436 mL | 1.3591 mL | |
| 50 mM | 0.0435 mL | 0.2174 mL | 0.4349 mL | 1.0872 mL | |
| 60 mM | 0.0362 mL | 0.1812 mL | 0.3624 mL | 0.9060 mL | |
| 80 mM | 0.0272 mL | 0.1359 mL | 0.2718 mL | 0.6795 mL | |
| 100 mM | 0.0217 mL | 0.1087 mL | 0.2174 mL | 0.5436 mL |
H052 Related Classifications
HY-173526 Related Classifications
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