| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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| ln Vitro |
MRT-83 demonstrates full antagonist capabilities, reducing ShhN (3 nM)-induced rat GCP growth with IC50 (~3 nM). MRT-83 also suppresses SAG (0.01 μM)-induced GCP growth (IC50 ~6 nM). MRT-83 prevents BC binding to HEK-hSmo cells in a dose-dependent manner with an IC50 of 4.6 nM. MRT-83 inhibits BC binding to cells expressing mouse Smo with an IC50 of 14 nM, which matches well with its IC50 in Shh-light2 and alkaline phosphatase assays [1].
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|---|---|
| ln Vivo |
The health of the animals treated with ShhN in the presence of MRT-83 was comparable to that of the other groups; however, there was no longer any evidence of Ptc transcription being upregulated in the SVZ of these animals, which is consistent with complete inhibition of ShhN-mediated effects (8.7 ±2.4 Ptc+ cells/section, n=9), which were not different from effects mediated by the vehicle. In vivo, ShhN-induced Ptc transcriptional upregulation in the LV SVZ can be inhibited by MRT-83 but not by MRT-36 [1].
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| References |
| Molecular Formula |
C31H30N4O5
|
|---|---|
| Molecular Weight |
538.59
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| Exact Mass |
538.221
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| CAS # |
1263131-92-5
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| Related CAS # |
MRT-83 hydrochloride;1359944-60-7
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| PubChem CID |
136210511
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| Appearance |
White to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.608
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| LogP |
5.23
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
40
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| Complexity |
841
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BKTMNLKJWHVZRN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H30N4O5/c1-19-10-15-24(33-31(32)35-30(37)23-16-26(38-2)28(40-4)27(17-23)39-3)18-25(19)34-29(36)22-13-11-21(12-14-22)20-8-6-5-7-9-20/h5-18H,1-4H3,(H,34,36)(H3,32,33,35,37)
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| Chemical Name |
3,4,5-trimethoxy-N-[N'-[4-methyl-3-[(4-phenylbenzoyl)amino]phenyl]carbamimidoyl]benzamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~464.17 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.86 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 20.8 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 | 1.8567 mL | 9.2835 mL | 18.5670 mL | |
| 5 mM | 0.3713 mL | 1.8567 mL | 3.7134 mL | |
| 10 mM | 0.1857 mL | 0.9284 mL | 1.8567 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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