Smurf1-IN-1
Based on 1 Customer Validation
Smurf1-IN-1 is an orally active and selective inhibitor of specific E3 ubiquitin protein ligase 1 (SMURF1) with an IC50 of 92 nM. Smurf1-IN-1 has significant efficacy in rats model of pulmonary hypertension.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.17%
- No. CAS: 1824708-03-3
- Fòrmula: C24H29ClN6O2
- Peso molecular:468.98
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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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
IC50: 92 nM Specific E3ubiquitin protein ligase 1 (SMURF1)[1]
In Vivo
Smurf1-IN-1 (1 mg/kg for i.v., 3 mg/kg for p.o.) shows a T1/2 of 7.9, and oral bioavailability of 82%[1].
Pharmacokinetic parameters for Smurf1-IN-1 (Compound 38) in rats [1]
| dose and route | oral bioavailability (%) | p.o. AUClast (nM • h /mL) | p.o. Cmax (nM/L) | half-life (h) | claearance (mL/min/kg) | Vss (1/kg) |
| 3 mpg p.o./1 mpg i.v. | 82 | 7383 | 2007 | 7.9 | 17.1 | 2.3 |
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (213.23 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 (5.33 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (5.33 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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 | 2.1323 mL | 10.6614 mL | 21.3229 mL | 53.3072 mL |
| 5 mM | 0.4265 mL | 2.1323 mL | 4.2646 mL | 10.6614 mL | |
| 10 mM | 0.2132 mL | 1.0661 mL | 2.1323 mL | 5.3307 mL | |
| 15 mM | 0.1422 mL | 0.7108 mL | 1.4215 mL | 3.5538 mL | |
| 20 mM | 0.1066 mL | 0.5331 mL | 1.0661 mL | 2.6654 mL | |
| 25 mM | 0.0853 mL | 0.4265 mL | 0.8529 mL | 2.1323 mL | |
| 30 mM | 0.0711 mL | 0.3554 mL | 0.7108 mL | 1.7769 mL | |
| 40 mM | 0.0533 mL | 0.2665 mL | 0.5331 mL | 1.3327 mL | |
| 50 mM | 0.0426 mL | 0.2132 mL | 0.4265 mL | 1.0661 mL | |
| 60 mM | 0.0355 mL | 0.1777 mL | 0.3554 mL | 0.8885 mL | |
| 80 mM | 0.0267 mL | 0.1333 mL | 0.2665 mL | 0.6663 mL | |
| 100 mM | 0.0213 mL | 0.1066 mL | 0.2132 mL | 0.5331 mL |
Smurf1-IN-1 Related Classifications
HY-149316 Related Classifications
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