1. GPCR/G Protein
  2. Cannabinoid Receptor
  3. WIN 55,212-2 Mesylate

WIN 55,212-2 Mesylate (Synonyms: (R)-(+)-WIN 55212)

Cat. No.: HY-13291 Purity: 99.01%
Handling Instructions

WIN 55,212-2 Mesylate is a potent aminoalkylindole cannabinoid (CB) receptor agonist with Kis of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively.

For research use only. We do not sell to patients.

WIN 55,212-2 Mesylate Chemical Structure

WIN 55,212-2 Mesylate Chemical Structure

CAS No. : 131543-23-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 69 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
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10 mg USD 84 In-stock
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50 mg USD 312 In-stock
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100 mg USD 552 In-stock
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Based on 5 publication(s) in Google Scholar

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Description

WIN 55,212-2 Mesylate is a potent aminoalkylindole cannabinoid (CB) receptor agonist with Kis of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively.

IC50 & Target

Ki: 62.3 nM (human recombinant CB1), 3.3 nM (human recombinant CB2)

In Vitro

WIN 55,212-2 is more potent in CHO-CB2 cells than in CHO-CB1 cells by a factor of 6O. WIN 55,212-2 has no effect on arachidonic acid release in CHO-CB2 or control CHO cells. WIN 55,212-2 fails to stimulate any increase in intracellular Ca2+ up to 10 μM[1]. In primary cultures of rat cerebral cortex neurons, WIN 55,212-2 (0.01--100 nM) increases extracellular glutamate levels, displaying a bell-shaped concentration-response curve. The facilitatory effect of WIN 55,212-2 (1 nM) is fully counteracted by SR141716A (10 nM), by the replacement of the normal Krebs Ringer-bicarbonate buffer with a low Ca2+ medium (0.2 mM) and by the IP(3) receptor antagonist xestospongin C (1 μM)[2]. WIN 55,212-2 evokes CGRP release from TG neurons in vitro (EC50=26 μM) in a concentration- and calcium-dependent manner. WIN 55,212-2-2 neither inhibits capsaicin-evokes CGRP release nor does it inhibit forskolin-, isoproteranol- or prostaglandin E2-stimulated cAMP accumulation. WIN 55,212-2 significantly inhibits (EC50=1.7 μM) 50 mm K+-evoked CGRP release by approximately 70%. WIN 55,212-2 inhibition of 50 mm K+-evoked CGRP release is not reversed by antagonists of cannabinoid type 1 (CB1) receptor, but is mimicks in magnitude and potency (EC50=2.7 μM) by its cannabinoid-inactive enantiomer WIN 55,212-2-3[3].

In Vivo

In the prefrontal cortex WIN 55,212-2 (0.1 and 1 mg/kg i.p.) increases dialysate glutamate levels from of the awake rat, while the lower (0.01 mg/kg) and the higher (2 mg/kg) doses are ineffective. Furthermore, the WIN 55,212-2 (0.1 mg/kg)- induced increase of dialysate glutamate levels is counteracted by pretreatment with the selective CB(1) receptor antagonist SR141716A (0.1 mg/kg, i.p.) and by the local perfusion with a low-calcium Ringer solution (Ca2+ 0.2 mM)[2]. WIN 55,212-2 (0.5, 1, 3, 5, 10 and 15 mg/kg, i.p.) does not alter the seizure threshold at low doses, while higher doses of the drug significantly increases the threshold in a dose-dependent manner. The anticonvulsant effect of WIN 55,212-2, which is observed with doses as high as 5 mg/kg, can be observed with doses as low as 0.5 mg/kg in groups pre-treated with 20 mg/kg of pioglitazone[4].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 34 mg/mL (65.06 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9135 mL 9.5674 mL 19.1347 mL
5 mM 0.3827 mL 1.9135 mL 3.8269 mL
10 mM 0.1913 mL 0.9567 mL 1.9135 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[3]

In experiment 1, different doses of WIN 55,212-2 (0.5, 1, 3, 5, 10 and 15 mg/kg) are injected 60 min prior to the determination of clonic seizure threshold induced by intravenous administration of PTZ solution. Control animals receive the same volume of the vehicle (1% aqueous solution of DMSO). The doses and time point are chosen on the basis of pilot studies. In experiment 2, in order to confirm the anticonvulsant effects of pioglitazone, different doses (10, 20, 40 and 80 mg/kg) are administered 4 h prior to PTZ in distinct groups of mice. The corresponding control groupreceive the appropriate vehicle (CMC 1%) at the same time point. In experiment 3, The additive anti epileptic effects of WIN 55,212-2 and pioglitazone are examined; mice receive acute administration of pioglitazone (10 or 20 mg/kg) 3 h before WIN 55,212-2 (0.5 or 1 mg/kg) and 4 h before PTZ.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

522.61

Formula

C₂₈H₃₀N₂O₆S

CAS No.

131543-23-2

SMILES

O=C(C1=C2C=CC=CC2=CC=C1)C3=C(N4[[email protected]@H](COC5=C4C3=CC=C5)CN6CCOCC6)C.CS(=O)(O)=O

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Product Name:
WIN 55,212-2 Mesylate
Cat. No.:
HY-13291
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WIN 55,212-2 Mesylate

Cat. No.: HY-13291