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Submit ReviewClocinnamox mesylate
Description: Irreversible μ antagonist
Alternative Names: NIH 10443, C-CAM
Chemical Name: 14β-(p-Chlorocinnamoylamino)-7,8-dihydro-N-cyclopropylmethylmorphinone mesylate
Purity: ≥98% (HPLC)
Biological Activity for Clocinnamox mesylate
Clocinnamox mesylate is a systemically active, irreversible μ-opioid receptor antagonist (apparent Ki values are 0.7, 1.9 and 5.7 nM for mouse μ, δ and κ receptors respectively).
Technical Data for Clocinnamox mesylate
| M. Wt | 601.11 |
| Formula | C29H29ClN2O4.CH3SO3H |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 117332-69-1 |
| PubChem ID | 90479744 |
| InChI Key | XAXNKAGAUFXFDO-JVJDXIHNSA-N |
| Smiles | C[S](O)(=O)=O.[H][C@@]12OC3=C4C(C[C@@]5([H])N(CC6CC6)CC[C@@]14[C@]5(CCC2=O)NC(=O)C=CC1=CC=C(Cl)C=C1)=CC=C3O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Clocinnamox mesylate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 60.11 | 100 | |
| ethanol | 15.03 | 25 |
Preparing Stock Solutions for Clocinnamox mesylate
The following data is based on the product molecular weight 601.11. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.66 mL | 8.32 mL | 16.64 mL |
| 5 mM | 0.33 mL | 1.66 mL | 3.33 mL |
| 10 mM | 0.17 mL | 0.83 mL | 1.66 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.33 mL |
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Product Datasheets for Clocinnamox mesylate
References for Clocinnamox mesylate
References are publications that support the biological activity of the product.
Aceto et al (1989) Very long-acting narcotic antagonists. The 14β-p-substituted cinnamoylaminomorphinones and their partial mu agonist codeinone relatives. Arzneimittelforschung 39 570 PMID: 2547389
Burke et al (1994) Irreversible opioid antagonist effects of clocinnamox on opioid analgesia and mu receptor binding in mice. J.Pharmacol.Exp.Ther. 271 715 PMID: 7965787
Zernig et al (1996) Mechanism of clocinnamox blockade of opioid receptors: evidence from in vitro and ex vivo binding and behavioural assays. J.Pharmacol.Exp.Ther. 279 23 PMID: 8858971
Broadbear et al (2000) Methocinnamox is a potent, long-lasting, and selective antagonist of morphine-mediated antinociception in the mouse: comparison with clocinnamox, β-funaltrexamine, and β-chlornaltrexamine. J.Pharmacol.Exp.Ther. 294 933 PMID: 10945843
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Keywords: Clocinnamox mesylate, Clocinnamox mesylate supplier, irreversible, mu-opioids, m-opioids, μ-opioids, receptors, antagonists, NIH, 10443, C-CAM, Mu, Opioid, Receptors, 0898, Tocris Bioscience
1 Citation for Clocinnamox mesylate
Citations are publications that use Tocris products. Selected citations for Clocinnamox mesylate include:
Sirohi et al (2008) The analgesic efficacy of fentanyl: relationship to tolerance and mu-opioid receptor regulation. Pharmacol Biochem Behav 91 115 PMID: 18640146
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