| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Dimemorfan phosphate (Astomin; AT17; Gentus; AT-17) is a morphinan-based sigma 1 receptor agonist with potent antitussive activity. It has been approved for use in Japan as well as in Spain and Italy.
| ln Vitro |
Dimemorfan (5–20 μM) is more effective at inhibiting the formation of ROS caused by fMLP (IC50 value of 7.0 μM) than that of PMA. It does so in a concentration-dependent way. When it comes to using the xanthine/xanthine oxidase system to scavenge free radicals, dimemorfan (10–50 μM) shows no discernible activity. Dimemorfan dramatically reduced the upregulation of Mac-1 in the groups that were activated by PMA and fMLP. Dimemorfan (10–20 μM) dramatically reduced the amount of ROS and NO produced by LPS, as well as the expression of the iNOS protein, the proportion of positive staining populations in the BV2 cytoplasm, and the MCF intensity of TNF-α and MCP-1. The degradation of cytoplasmic Iκ-Bα, nuclear translocation of NF-κB p65, and transcriptional activity of NF-κB are all markedly inhibited by dimemorfan (20 μM) [2].
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| ln Vivo |
The dose-related reduction of BAY k-8644-induced convulsive behavior was seen with dimemorfan (6.25 or 12.5 mg/kg, sc) (6.25 mg/kg dimemorfan+BAY k-8644 or 12.5 mg/kg dimemorfan+BAY k-8644 vs. Compared with saline+BAY k-8644, P<0.05 and P<0.01, respectively). In a dose-dependent manner, dimemorfan dramatically reduced the rise in c-fos and c-jun protein expression that was caused by BAY k-8644. Mice's locomotor activity was not significantly affected by dimemofan, and no discernible circling behavior was observed in any movement pattern [1]. Dimemorfan, administered intraperitoneally at doses of 1 and 5 mg/kg, prevents mice's plasma levels of TNF-α from rising. Dimemorfan administration effectively decreased both the neutrophil infiltration into the liver and lungs as well as the LPS-induced development of oxidative stress (EB staining) in these tissues [2].
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| References |
[1]. Shin EJ, et al. Dimemorfan prevents seizures induced by the L-type calcium channel activator BAY k-8644 in mice. Behav Brain Res. 2004 May 5;151(1-2):267-76.
[2]. Wang YH, et al. Anti-inflammatory effects of dimemorfan on inflammatory cells and LPS-induced endotoxin shock in mice. Br J Pharmacol. 2008 Jul;154(6):1327-38 |
| Molecular Formula |
C18H25N.H3O4P
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|---|---|
| Molecular Weight |
353.39302
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| CAS # |
36304-84-4
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| Related CAS # |
36304-84-4 (phosphate);36304-82-2;
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| SMILES |
O=P(O)(O)O.CN1[C@](CC2=CC=C(C)C=C32)([H])[C@](CCCC4)([H])[C@]34CC1
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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) |
H2O : ~10 mg/mL (~28.30 mM)
DMSO : ~1 mg/mL (~2.83 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 16.67 mg/mL (47.17 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8297 mL | 14.1487 mL | 28.2973 mL | |
| 5 mM | 0.5659 mL | 2.8297 mL | 5.6595 mL | |
| 10 mM | 0.2830 mL | 1.4149 mL | 2.8297 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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