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WIN-55212-2 mesylate

  Cat. No.:  DC2050   Featured
Chemical Structure
131543-23-2
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Field of application
WIN 55212-2 (mesylate) is a potent aminoalkylindole cannabinoid (CB) receptor agonist with a Ki of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 131543-23-2
Chemical Name: WIN552122,WIN-552122
Synonyms: WIN552122,WIN-552122
SMILES: C([C@@H]1C(CN2CCOCC2)N2C(C)=CC3=C2C(=CC=C3)O1)(C1=C2C(C=CC=C2)=CC=C1)=O.OS(C)(=O)=O
Formula: C28H30N2O6S
M.Wt: 522.61
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
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.
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].
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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC1076 Otenabant(CP945598.HCl) CP-945598 HCl is a potent and selective cannabinoid type 1 receptor antagonist with Ki of 0.7 nM.
DC2050 WIN-55212-2 mesylate WIN 55212-2 (mesylate) is a potent aminoalkylindole cannabinoid (CB) receptor agonist with a Ki of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively.
DC8887 Pravadoline(WIN 48,098) Pravadoline is a cannabimimetic aminoalkylindole agonist of the cannabinoid receptors and an inhibitor of Cox-1 and Cox-2, demonstrating powerful analgesic effects through the combination of these actions.
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DC7109 Otenabant (CP-945598 free base) Otenabant (CP945598) is a recently discovered selective, high affinity, competitive CB1 receptor antagonist with Ki of 0.7 nM.
DC12081 LY2828360 LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
DC10095 JD5037 JD5037 is an inverse agonist of peripheral cannabinoid 1 (CB1) receptors (Ki = 0.35 nM).
DC7840 BML-190 BML-190 is an indomethacin morpholinylamide which functions as a selective inverse agonist of the human cannabinoid CB2 receptor.
DC9783 Bay 59-3074 Bay 59-3074 is a novel CB1/CB2 receptor partial agonist (Ki values are 48.3 and 45.5 nM at human CB1 and CB2 receptors respectively).
DC8886 Iodopravadoline(AM-630) AM630 is a selective CB2 receptor antagonist that binds to CB1 and CB2 receptors with Ki values of 5.2 µM and 31.2 nM, respectively.
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