ASK1-IN-2
Based on 1 Customer Validation
ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.37%
- No. CAS: 2541792-70-3
- Fòrmula: C19H17FN6O
- Peso molecular:364.38
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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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Apoptosis Compound Library
HY-L003
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Immunology/Inflammation Compound Library
HY-L007
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Kinase Inhibitor Library
HY-L009
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MAPK Compound Library
HY-L010
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Oxygen Sensing Compound Library
HY-L045
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Orally Active Compound Library
HY-L061
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Anti-Obesity Compound Library
HY-L087
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Targeted Diversity Library
HY-L099
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Heterocyclic Compound Library
HY-L138
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Highly Selective Inhibitors Library
HY-L158
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Cell Death Library
HY-L162
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Serine/Threonine Kinase Inhibitor Library
HY-L164
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Anti-Fibrosis Compound Library
HY-L185
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
Ver todos los productos específicos de isoformas MAP3K
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Actividad biológica
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ASK1 32.8 nM (IC50) |
ASK1-IN-2 (compound 19) (10 mM; 1 h) inhibits the luciferase reporter activity in AP1-HEK293 cells, with inhibition rate of 95.59%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) blocks ASK1-p38/JNK signaling pathways and reduces inflammatory cytokine levels in DSS-induced mouse colon tissues[1].
ASK1-IN-2 (1 mg/kg; i.v.) shows low clearance (CL=1.38 L/h/kg) and moderate half-life (T1/2=1.45 h) in rats[1].
ASK1-IN-2 (10 mg/kg; p.o.) shows high oral exposure (AUClast=4517 h ng/mL), 62.2% oral bioavailability and acceptable terminal half-life (T1/2=2.31 h) in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ICR mice (18-22 g, 6-8 weeks) were given 3% DSS (w/v) orally in drinking water[1]
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Dosage:25 mg/kg
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Administration:P.o. daily for 7 days
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Result:Induced a significant recovery of body weight loss, with an increase of +11.2%.
Decreased the disease activity index (DAI) score about a 2 unit.
Significantly prevented colon shortening.
Attenuated a severe colonic tissue damage and infiltration of inflammatory cells.
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Animal Model:Male SD rats [1]
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Dosage:1 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
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Administration:I.v. and p.o. administration
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Result:I.v.: CL=1.38 L/h/kg; T1/2=1.45 h.
P.o.: AUClast=4517 h•ng/mL; F=62.2%; T1/2=2.31 h.
Chemical Information
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No. CAS 2541792-70-3
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Appearance Solid
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Peso molecular 364.38
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Fòrmula C19H17FN6O
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Color White to off-white
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SMILES
O=C(C(N1)=CC2=C1C=C(F)C=C2)NC3=NC(C4=NN=CN4C(C)C)=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 : 250 mg/mL (686.10 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: ≥ 2.08 mg/mL (5.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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 (274 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7444 mL | 13.7219 mL | 27.4439 mL | 68.6097 mL |
| 5 mM | 0.5489 mL | 2.7444 mL | 5.4888 mL | 13.7219 mL | |
| 10 mM | 0.2744 mL | 1.3722 mL | 2.7444 mL | 6.8610 mL | |
| 15 mM | 0.1830 mL | 0.9148 mL | 1.8296 mL | 4.5740 mL | |
| 20 mM | 0.1372 mL | 0.6861 mL | 1.3722 mL | 3.4305 mL | |
| 25 mM | 0.1098 mL | 0.5489 mL | 1.0978 mL | 2.7444 mL | |
| 30 mM | 0.0915 mL | 0.4574 mL | 0.9148 mL | 2.2870 mL | |
| 40 mM | 0.0686 mL | 0.3430 mL | 0.6861 mL | 1.7152 mL | |
| 50 mM | 0.0549 mL | 0.2744 mL | 0.5489 mL | 1.3722 mL | |
| 60 mM | 0.0457 mL | 0.2287 mL | 0.4574 mL | 1.1435 mL | |
| 80 mM | 0.0343 mL | 0.1715 mL | 0.3430 mL | 0.8576 mL | |
| 100 mM | 0.0274 mL | 0.1372 mL | 0.2744 mL | 0.6861 mL |
ASK1-IN-2 Related Classifications
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