Clocinnamox mesylate

Name: Clocinnamox mesylate
Brand: Tocris Bioscience
SKU: 0898

Catalog # 0898

Citations (1)

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Key Product Details

Description:	Irreversible μ antagonist
Alternative Names:	NIH 10443, C-CAM
Chemical Name:	14β-(p-Chlorocinnamoylamino)-7,8-dihydro-N-cyclopropylmethylmorphinone mesylate
Purity:	≥98% (HPLC)
Molecular Weight:	601.11

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Biological Activity

Clocinnamox mesylate is a systemically active, irreversible μ-opioid receptor antagonist (apparent K_i 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-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

	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 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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References

References are publications that support the biological activity of the product.

Broadbear 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. 2000 PMID: 10945843
Zernig Mechanism of clocinnamox blockade of opioid receptors: evidence from in vitro and ex vivo binding and behavioural assays. J.Pharmacol.Exp.Ther. 1996 PMID: 8858971
Burke Irreversible opioid antagonist effects of clocinnamox on opioid analgesia and mu receptor binding in mice. J.Pharmacol.Exp.Ther. 1994 PMID: 7965787
Aceto Very long-acting narcotic antagonists. The 14β-p-substituted cinnamoylaminomorphinones and their partial mu agonist codeinone relatives. Arzneimittelforschung 1989 PMID: 2547389

Citations for Clocinnamox mesylate (1)

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Citations are publications that use Bio-Techne 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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