Home GPCR & G Protein Cannabinoid Receptor agonist WIN 55, 212-2 mesylate

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WIN 55, 212-2 mesylate Cannabinoid Receptor agonist

Cat.No.S8017

WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent cannabinoid (CB) receptor agonist with Ki of 3.3 nM and 62.3 nM for human recombinant CB2 and CB1, respectively. WIN 55,212-2 Mesylate regulates Glutamate transmission.
WIN 55, 212-2 mesylate Cannabinoid Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 522.61

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Quality Control

Chemical Information, Storage & Stability

Molecular Weight 522.61 Formula

C28H30N2O6S

 Storage (From the date of receipt)
CAS No. 131543-23-2 -- Storage of Stock Solutions

Synonyms (R)-(+)-WIN 55212 Smiles CC1=C(C2=C3N1C(COC3=CC=C2)CN4CCOCC4)C(=O)C5=CC=CC6=CC=CC=C65.CS(=O)(=O)O

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (191.34 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
CB2 [2]
(Cell-free assay)
3.3 nM(Ki)
CB1 [2]
(Cell-free assay)
62.3 nM(Ki)
In vitro

WIN 55,212-2 increases, in a nanomolar concentration range, extra-cellular glutamate levels in primary cultures of rat cerebral cortex neurons, displaying a bell-shaped concentration-response curve.[1] The aminoalkylindole WIN 55,212-2 is more selective for the CB2 than the CB1 receptor, with a CB2-to-CB1 dose-response ratio of 19.[2]
In vivo

The result provide in vivo evidence for CB1 receptor-mediated increase on endogenous glutamate levels in the cerebral cortex. The cannabinoid receptor agonist WIN 55,212-2, at low mg/kg doses, enhances dialysate glutamate levels in the prefrontal cortex of the awake rat.[1]
References

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