WIN 55, 212-2 mesylate

Catalog No.S8017 Batch:S801701

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Technical Data

Formula

C28H30N2O6S
Molecular Weight 522.61 CAS No. 131543-23-2
Solubility (25°C)* In vitro DMSO 100 mg/mL (191.34 mM)
Ethanol 20 mg/mL (38.26 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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.
Targets
CB2 [2]
(Cell-free assay)		 CB1 [2]
(Cell-free assay)
3.3 nM(Ki) 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]
Density g/mL

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    cerebral cortical cells

  • Concentrations

    1 nM, 10 nM

  • Incubation Time

    15 min

  • Method

    On the day of the release experiment, the cells are rinsed twice by replacing the culture medium with Krebs Ringer-bicarbonate buffer (37℃). Thereafter, five consecutive fractions are collected, renewing this solution (400μl) every 30 min. The first 2 samples are used to assess basal glutamate levels, while pharmacological treatments are carried out during the third fraction. WIN 55,212-2 is applied 15 min before the end of the third fraction.
Animal Study:

[1]
  • Animal Models

    male adult sprague-dawley rats

  • Dosages

    0.01 mg/kg - 2 mg/kg

  • Administration

    IP

Selleck's WIN 55, 212-2 mesylate has been cited by 1 publication

Gut-microbiota-brain axis in the vulnerability to psychosis in adulthood after repeated cannabis exposure during adolescence [ Eur Arch Psychiatry Clin Neurosci, 2022, 10.1007/s00406-022-01437-1] PubMed: 35666299

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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