research use only
Cat.No.S8017
| Related Targets | CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas |
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| Other Cannabinoid Receptor Inhibitors | AM1241 AM251 BML-190 Otenabant (CP-945598) HCl 6-Iodopravadoline (AM630) Org 27569 GW842166X CID16020046 Yangonin (+)-Gallocatechin |
| Molecular Weight | 522.61 | Formula | C28H30N2O6S |
Storage (From the date of receipt) | |
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| CAS No. | 131543-23-2 | -- | Storage of Stock Solutions |
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| 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 | ||
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In vitro |
DMSO
: 100 mg/mL
(191.34 mM)
Water : 100 mg/mL Ethanol : 100 mg/mL |
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In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
| Targets/IC50/Ki |
CB2
(Cell-free assay) 3.3 nM(Ki)
CB1
(Cell-free assay) 62.3 nM(Ki)
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| 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. 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. |
| In vivo |
The results 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. |
References |
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