| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
The size of Jurkat cells is lowered by NR1 (1–10 μM; 48 hours) [1]. MCF-7, TRI102, and PC3 cells are exposed to NR1 (0.37-30 μM) for 90 minutes, which inhibits phosphorylation of T389pS6K1, and promotes phosphorylation of S473pAKT [1]. MCF-7 protein synthesis is decreased by NR1 (1-30 μM; 2.5 h)[1].
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|---|---|
| ln Vivo |
In kidney and skeletal muscle, NR1 (30 mg/kg; i.p.; single dosage) markedly decreased mTORC1 activity and in skeletal muscle, it demonstrated a substantial band shift of T37/464E-BP1 [1].
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| Cell Assay |
Cell Viability Assay [1]
Cell Types: Jurkat Cells Tested Concentrations: 1, 3 and 10 μM Incubation Duration: 48 hrs (hours) Experimental Results: Effectively diminished the size of Jurkat cells in a dose-dependent manner. Western Blot Analysis[1] Cell Types: MCF-7, TRI102 and PC3 Cell Tested Concentrations: 0.37, 1.1, 3.3, 10 and 30 μM Incubation Duration: MCF-7 and TRI102 90 minutes; 24 hrs (hours) PC3 Experimental Results: in a dose-dependent manner Inhibits the phosphorylation of T389pS6K1 and increases the phosphorylation of S473pAKT. Western Blot Analysis[1] Cell Types: MCF-7 Tested Concentrations: 1, 3, 10 and 30 μM Incubation Duration: 2.5 hrs (hours) (cells were then labeled with 35S-Met labeling mixture for 30 minutes) Experimental Results: Dose-dependent reduction in protein synthesis. |
| Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice (6-7 weeks; 16 hrs (hrs (hours)) fasted) [1]
Doses: 30 mg/kg Route of Administration: IP; Single Dose Experimental Results: Over 5 µM for 2 hrs (hrs (hours)). mTORC1 activity in kidney and skeletal muscle was Dramatically diminished, and T37/464E-BP1 in skeletal muscle demonstrated obvious band shifting. |
| References |
| Molecular Formula |
C25H19BRCL2N2O3S
|
|---|---|
| Molecular Weight |
578.304962396622
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| Exact Mass |
575.967
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| CAS # |
2216763-38-9
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| PubChem CID |
132281917
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| Appearance |
White to off-white solid powder
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| LogP |
6.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
34
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| Complexity |
739
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| Defined Atom Stereocenter Count |
0
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| SMILES |
BrC1=CC(=CC2=C1C=C(C(=O)O)N2CC1C=CC(C(N(C)C)=O)=CC=1)SC1C=CC(=C(C=1)Cl)Cl
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| InChi Key |
MJYFVDNMTKLGTH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H19BrCl2N2O3S/c1-29(2)24(31)15-5-3-14(4-6-15)13-30-22-11-17(34-16-7-8-20(27)21(28)10-16)9-19(26)18(22)12-23(30)25(32)33/h3-12H,13H2,1-2H3,(H,32,33)
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| Chemical Name |
4-bromo-6-(3,4-dichlorophenyl)sulfanyl-1-[[4-(dimethylcarbamoyl)phenyl]methyl]indole-2-carboxylic acid
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| Synonyms |
NR 1; NR-1; NR1
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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)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~86.46 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7292 mL | 8.6459 mL | 17.2918 mL | |
| 5 mM | 0.3458 mL | 1.7292 mL | 3.4584 mL | |
| 10 mM | 0.1729 mL | 0.8646 mL | 1.7292 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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