ASM-IN-1
Based on 1 Customer Validation
ASM-IN-1 is a potent and orally active acid sphingomyelinase (ASM) inhibitor with an IC50 value of 1.5 µM. ASM-IN-1 reduces lipid plaques in the aortic arch and aorta and reduces plasma ceramide concentration and Ox-LDL levels. ASM-IN-1 shows antiatherosclerotic and anti-inflammatory activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.65%
- No. CAS: 2913151-46-7
- Fòrmula: C16H12BrN3O4
- Peso molecular:390.19
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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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Actividad biológica
ASM-IN-1 (compound 4i) (0-20 µM) dose not affect cell growth in HUVECs[1].
ASM-IN-1 (0, 1, 5 µM) reduces the expressions of IL-6 and TNF-α with LPS stimulated in a dose-dependent manner, decreases the expression of MCP-1 mRNA in HUVECs[1].
ASM-IN-1 (5 µM) reduces Ox-LDL-stimulated MCP-1 mRNA expression and restore IL-6 mRNA to a normal level[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HUVECs
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Concentration:0.5, 1, 5, 10, 20 µM
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Incubation Time:24, 48 h
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Result:Showed no affect on cell growth.
ASM-IN-1 (6, 12, 40 mg/kg; i.p.; twice a day for 8 weeks) antiatherosclerotic activity by inhibiting ASM in mice[1].
Pharmacokinetic Parameters of ASM-IN-1 in ICR mice[1].
| parameter | iv | po |
| T1/2 (h) | 0.20 ± 0.04 | 0.83 ± 0.32 |
| Tmax (h) | 0.083 ± 0.00 | 0.083 ± 0.00 |
| Cmax (ng/mL) | 787 ± 64.7 | 2763 ± 485 |
| AUC0-t (h·ng/mL) | 227 ± 14.3 | 805 ± 76.7 |
| AUC0-∞ (h·ng/mL) | 228 ± 15.1 | 809 ± 75.1 |
| Vz (mL/kg) | 1277 ± 216 | |
| CL (mL/h/kg) | 4390 ± 291 | |
| MRT0-t (h) | 0.077 ± 0.012 | 0.32 ± 0.078 |
| MRT0-∞ (h) | 0.087 ± 0.019 | 0.35 ± 0.064 |
| F (%) | 35.42 ± 0.033% |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2913151-46-7
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Appearance Solid
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Peso molecular 390.19
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Fòrmula C16H12BrN3O4
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Color White to off-white
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SMILES
BrC1=CC=C(OCC2=CC=C(C3=NOC(C(NO)=O)=N3)C=C2)C=C1
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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 : 60 mg/mL (153.77 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.
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 (275 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 | 2.5629 mL | 12.8143 mL | 25.6285 mL | 64.0713 mL |
| 5 mM | 0.5126 mL | 2.5629 mL | 5.1257 mL | 12.8143 mL | |
| 10 mM | 0.2563 mL | 1.2814 mL | 2.5629 mL | 6.4071 mL | |
| 15 mM | 0.1709 mL | 0.8543 mL | 1.7086 mL | 4.2714 mL | |
| 20 mM | 0.1281 mL | 0.6407 mL | 1.2814 mL | 3.2036 mL | |
| 25 mM | 0.1025 mL | 0.5126 mL | 1.0251 mL | 2.5629 mL | |
| 30 mM | 0.0854 mL | 0.4271 mL | 0.8543 mL | 2.1357 mL | |
| 40 mM | 0.0641 mL | 0.3204 mL | 0.6407 mL | 1.6018 mL | |
| 50 mM | 0.0513 mL | 0.2563 mL | 0.5126 mL | 1.2814 mL | |
| 60 mM | 0.0427 mL | 0.2136 mL | 0.4271 mL | 1.0679 mL | |
| 80 mM | 0.0320 mL | 0.1602 mL | 0.3204 mL | 0.8009 mL | |
| 100 mM | 0.0256 mL | 0.1281 mL | 0.2563 mL | 0.6407 mL |
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