| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
In HEK293 cells, MRT-10 suppresses the Smo-induced IP accumulation in a dose-dependent manner (IC50=2.5 μM)[1]. With an IC50=0.5 μM, MRT-10 (10-9-10-5 M; 2 h) inhibits the binding of bodipy-cyclopamine (5 nM; 2 h) to cells expressing mouse Smo in a dose-dependent manner[1]. MRT-10 (10-9-10-5 M; 40 h) has an IC50=0.64 μM and suppresses ShhN signaling in Shh-light2 cells in a dose-dependent manner[1]. MRT-10 (10-9-10-5 M; 6 days) suppresses the alkaline phosphatase (AP) activity in C3H10T1/2 cells that is stimulated by SAG (0.1 μM) (IC50=0.90 μM).
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| References |
[1]. Manetti F, et al. Virtual screening-based discovery and mechanistic characterization of the acylthiourea MRT-10 family as smoothened antagonists. Mol Pharmacol. 2010 Oct;78(4):658-65.
[2]. Solinas A, et al. Acylthiourea, acylurea, and acylguanidine derivatives with potent hedgehog inhibiting activity. J Med Chem. 2012 Feb 23;55(4):1559-71. |
| Molecular Formula |
C24H23N3O5S
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|---|---|
| Molecular Weight |
465.52
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| CAS # |
330829-30-6
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| SMILES |
C(NC1=CC=CC(NC(NC(=O)C2C=C(OC)C(OC)=C(OC)C=2)=S)=C1)(=O)C1C=CC=CC=1
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (214.81 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1481 mL | 10.7407 mL | 21.4814 mL | |
| 5 mM | 0.4296 mL | 2.1481 mL | 4.2963 mL | |
| 10 mM | 0.2148 mL | 1.0741 mL | 2.1481 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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