WIN 55,212-3 mesylate
Novel, low potency CB2 receptor silent antagonist and CB1 receptor partial inverse agonist. Competitively antagonizes effects of CP 55,940 (pA2 = 6.1) and SR 144528 (pEC50 = 5.3) at CB2 receptors and acts as a partial inverse agonist at CB1 receptors (pIC50 = 5.5). Displays modest activity at human melatonin MT1 and muscarinic M4 receptors, but is selective over several other GPCRs.
R-enantiomer also available.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|DMSO||52.26||100mM with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 522.61. 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.91 mL||9.57 mL||19.13 mL|
|5 mM||0.38 mL||1.91 mL||3.83 mL|
|10 mM||0.19 mL||0.96 mL||1.91 mL|
|50 mM||0.04 mL||0.19 mL||0.38 mL|
References are publications that support the products' biological activity.
Savinainen et al (2005) Identification of WIN55212-3 as a competitive neutral antagonist of the human cannabinoid CB2 receptor. Br.J.Pharmacol. 145 636 PMID: 15852035
If you know of a relevant reference for WIN 55,212-3 mesylate, please let us know.
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Keywords: WIN 55,212-3 mesylate, supplier, CB2, antagonists, CB1, partial, inverse, agonists, cannabinoids, Non-Selective, Receptors, WIN552123, mesylate, (S)-(-)-WIN55212, cb2r, cb1r, (S)-(-)-WIN, 55,212, Non-selective, Cannabinoids, Non-selective, Cannabinoids, Tocris Bioscience
2 Citations for WIN 55,212-3 mesylate
Citations are publications that use Tocris products. Selected citations for WIN 55,212-3 mesylate include:
Mereu et al (2003) Prenatal exposure to a cannabinoid agonist produces memory deficits linked to dysfunction in hippocampal long-term potentiation and glutamate release. Proc Natl Acad Sci U S A 100 4915 PMID: 12679519
Sousa et al (2011) Regulation of hippocampal cannabinoid CB1 receptor actions by adenosine A1 receptors and chronic caffeine administration: implications for the effects of δ9-tetrahydrocannabinol on spatial memory. Neuropsychopharmacology 36 472 PMID: 20927050
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Literature in this Area
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