MRT-81
Based on 1 Customer Validation
MRT-81 is a potent antagonist of human and rodent smoothened (Smo) receptors, with an IC50 value of 41 nM in the Shh-light2 cells. MRT-81 has potent hedgehog inhibiting activity. MRT-81 can be used for the research of cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.85%
- No. CAS: 1263132-08-6
- Fòrmula: C31H29N3O5S
- Peso molecular:555.64
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
Actividad biológica
IC50: 41 nM (Shh-light2 cells Smo receptors)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| C3H 10T1/2 | IC50 |
0.06 μM
Compound: 61
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Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs
Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs
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[PMID: 22268551] |
| HEK293 | IC50 |
63 nM
Compound: 61
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Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy
Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy
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[PMID: 22268551] |
| Shh Light II | IC50 |
0.041 μM
Compound: 61
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Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay
Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay
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[PMID: 22268551] |
MRT-81 inbihits the differentiation of the mesenchymal pluripotent C3H10T1/2 cells into alkaline phosphatasepositive osteoblasts induced by the Smo agonist SAG (0.1 μM), with an IC50 value of 64 nM[1].
MRT-81 (1-1000 nM) is a potent antagonist of SAG (0.01 μM)-induced proliferation of rat granule cell precursors (GCPs) with an IC50 less than 10 nM[1].
MRT-81 (0, 0.1, 1, 10, 30, 100, 300, 1000 nM; 2 h; 37 °C) blocks BODIPY-cyclopamine (5 nM) binding to hSmo in a dose-dependent manner with an IC50 of 63 nM in HEK-hSmo cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1263132-08-6
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Appearance Solid
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Peso molecular 555.64
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Fòrmula C31H29N3O5S
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Color White to light yellow
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SMILES
O=C(C1=CC=C(C2=CC=CC=C2)C=C1)NC3=CC(NC(NC(C4=CC(OC)=C(C(OC)=C4)OC)=O)=S)=CC=C3C
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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 (179.97 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 (270 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 | 1.7997 mL | 8.9986 mL | 17.9973 mL | 44.9932 mL |
| 5 mM | 0.3599 mL | 1.7997 mL | 3.5995 mL | 8.9986 mL | |
| 10 mM | 0.1800 mL | 0.8999 mL | 1.7997 mL | 4.4993 mL | |
| 15 mM | 0.1200 mL | 0.5999 mL | 1.1998 mL | 2.9995 mL | |
| 20 mM | 0.0900 mL | 0.4499 mL | 0.8999 mL | 2.2497 mL | |
| 25 mM | 0.0720 mL | 0.3599 mL | 0.7199 mL | 1.7997 mL | |
| 30 mM | 0.0600 mL | 0.3000 mL | 0.5999 mL | 1.4998 mL | |
| 40 mM | 0.0450 mL | 0.2250 mL | 0.4499 mL | 1.1248 mL | |
| 50 mM | 0.0360 mL | 0.1800 mL | 0.3599 mL | 0.8999 mL | |
| 60 mM | 0.0300 mL | 0.1500 mL | 0.3000 mL | 0.7499 mL | |
| 80 mM | 0.0225 mL | 0.1125 mL | 0.2250 mL | 0.5624 mL | |
| 100 mM | 0.0180 mL | 0.0900 mL | 0.1800 mL | 0.4499 mL |
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