| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| ln Vitro |
The extracellular signal-regulated kinase (ERK1/2) pathway is inhibited by CFM-2. CFM-2 upregulates tumor suppressor protein p21 and cell cycle regulatory factors while decreasing the phosphorylation of cAMP response element binding protein (CREB) and inhibiting the expression of cyclin D1. and p53 resulted in a drop in the proportion of lung adenocarcinoma cells in the G2 and S cell cycle stages.
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| ln Vivo |
CFM-2 pretreatment slows the advancement of seizure grade when pentylenetetrazole is administered repeatedly. The mean epilepsy score at the end of the 6-week repeated pentylenetetrazole treatment period was 0 in the vehicle-treated controls, 4.3 in the animals treated with vehicle + pentylenetetrazole (treated with CFM-2 (20 μmol/kg; peritoneal 2.2) + pentylenetetrazole in rats chronically treated (intravenous injection), and 1.0 in rats repeatedly treated with CFM-2 (50 μmol/kg; i.p.) + pentylenetetrazole). In pentylenetetrazole-kindled animals, CFM-2 can likewise counteract the long-term increase in sensitivity to the convulsive effects of GABA function inhibitors [1]. The ipsilateral hind paw's mechanical and thermal hypersensitivity was considerably reduced at two and twenty-four hours following CFA injection by intrathecal administration of two selective noncompetitive AMPAR antagonists, CFM-2 (25 and 50 μg) and GYKI 52466 (50 μg). hypersensitivity response. When subjected to mechanical and thermal stimulation, the contralateral basal response is unaffected by either GYKI 52466 or CFM-2 [4].
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| References |
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| Additional Infomation |
1-(4-aminophenyl)-7,8-dimethoxy-3,5-dihydro-2,3-benzodiazepin-4-one is a benzodiazepine.
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| Molecular Formula |
C17H17N3O3
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|---|---|
| Molecular Weight |
311.33518
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| Exact Mass |
311.127
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| CAS # |
178616-26-7
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| PubChem CID |
4377504
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| Appearance |
Light yellow to khaki solid powder
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| Density |
1.32g/cm3
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| Index of Refraction |
1.637
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| LogP |
2.056
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
460
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MJKADKZSYQWGLL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17N3O3/c1-22-14-7-11-8-16(21)19-20-17(13(11)9-15(14)23-2)10-3-5-12(18)6-4-10/h3-7,9H,8,18H2,1-2H3,(H,19,21)
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| Chemical Name |
1-(4-aminophenyl)-7,8-dimethoxy-3,5-dihydro-2,3-benzodiazepin-4-one
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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 : ≥ 50 mg/mL (~160.60 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (8.83 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 27.5 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 | 3.2119 mL | 16.0596 mL | 32.1192 mL | |
| 5 mM | 0.6424 mL | 3.2119 mL | 6.4238 mL | |
| 10 mM | 0.3212 mL | 1.6060 mL | 3.2119 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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