HS271
Based on 1 Customer Validation
HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.92%
- No. CAS: 2410393-15-4
- Fòrmula: C21H24F3N5O2
- Peso molecular:435.44
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Immunology/Inflammation Compound Library
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Orally Active Compound Library
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Posttranslational Modification Library
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Actividad biológica
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IRAK4 7.2 μM (IC50) |
HS271 exhibits a t1/2 of 3.3 h and Cmax of 2107 ng/mL[1].
HS271 is stable in liver microsome assays across other species, including rat, mouse, monkey, and human[1].
HS271 exhibits oral bioavailability of 67.3%, 58.2%, 14.4&% and 49% in mouse, rat, dog and monkey, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A rat model of collagen induced arthritis (CIA)[1].
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Dosage:15, 50, 150 mg/kg.
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Administration:PO, once daily.
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Result:Led to a significant reduction in paw swelling as compared to vehicle control, with a minimum effective dose at 15 mg/kg QD. Notably, at 150 mg/kg QD, HS271 eliminated the paw swelling.
Chemical Information
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No. CAS 2410393-15-4
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Appearance Solid
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Peso molecular 435.44
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Fòrmula C21H24F3N5O2
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Color White to yellow
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SMILES
O=C(NC1=CC2=CN(CCN(C)C)N=C2C=C1C(C)(O)C)C3=NC(C(F)(F)F)=CC=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (229.65 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)
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 (5.74 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 (5.74 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.
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.
Pureza y Documentación
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Ficha de datos (273 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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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.2965 mL | 11.4826 mL | 22.9653 mL | 57.4132 mL |
| 5 mM | 0.4593 mL | 2.2965 mL | 4.5931 mL | 11.4826 mL | |
| 10 mM | 0.2297 mL | 1.1483 mL | 2.2965 mL | 5.7413 mL | |
| 15 mM | 0.1531 mL | 0.7655 mL | 1.5310 mL | 3.8275 mL | |
| 20 mM | 0.1148 mL | 0.5741 mL | 1.1483 mL | 2.8707 mL | |
| 25 mM | 0.0919 mL | 0.4593 mL | 0.9186 mL | 2.2965 mL | |
| 30 mM | 0.0766 mL | 0.3828 mL | 0.7655 mL | 1.9138 mL | |
| 40 mM | 0.0574 mL | 0.2871 mL | 0.5741 mL | 1.4353 mL | |
| 50 mM | 0.0459 mL | 0.2297 mL | 0.4593 mL | 1.1483 mL | |
| 60 mM | 0.0383 mL | 0.1914 mL | 0.3828 mL | 0.9569 mL | |
| 80 mM | 0.0287 mL | 0.1435 mL | 0.2871 mL | 0.7177 mL | |
| 100 mM | 0.0230 mL | 0.1148 mL | 0.2297 mL | 0.5741 mL |
HS271 Related Classifications
HY-131903 Related Classifications
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