Clocinnamox mesylate

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Cat.No. 0898 - Clocinnamox mesylate | C29H29ClN2O4.CH3SO3H | CAS No. 117332-69-1
Description: Irreversible μ antagonist
Alternative Names: NIH 10443, C-CAM
Chemical Name: 14β-(p-Chlorocinnamoylamino)-7,8-dihydro-N-cyclopropylmethylmorphinone mesylate
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

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

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-XDZPJBHRSA-N
Smiles CS(=O)(O)=O.OC1=C(O5)C([C@]([C@@H]5C(CC3)=O)4[C@]3(NC(/C=C/C6=CC=C(Cl)C=C6)=O)C(N(CC7CC7)CC4)C2)=C2C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 60.11 100
ethanol 15.03 25

Preparing Stock Solutions

The following data is based on the product molecular weight 601.11. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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, supplier, irreversible, mu-opioids, m-opioids, μ-opioids, receptors, antagonists, NIH, 10443, C-CAM, Mu, Opioid, Receptors, Tocris Bioscience

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