Item no. |
S2778-5 |
Manufacturer |
Selleckchem
|
CASRN |
666260-75-9 |
Amount |
5 mg |
Category |
|
Type |
Inhibitors |
Specific against |
other |
ECLASS 10.1 |
32160490 |
ECLASS 11.0 |
32160490 |
UNSPSC |
12000000 |
Alias |
CB2;Cannabinoid Receptor |
Similar products |
GW-842166X |
Available |
|
Administration |
Orally administrated once daily for 8 days |
Animal Models |
rat model of neuropathic pain |
Chemical Name |
2-(2, 4-dichlorophenylamino)-N-((tetrahydro-2H-pyran-4-yl)methyl)-4-(trifluoromethyl)pyrimidine-5-carboxamide |
Clinical Trials |
GW842166X has finished phase I study in healthy subjects to investigate the distribution of GW842166X in the brain. |
Description |
GW842166X is a potent and highly selective agonist of CB2 receptor. |
Dosages |
15 mg/kg |
Features |
GW842166X has selective affinity for CB2 than CB1. |
Formulation |
saline |
IC50 |
63 nM [1], 63 nM [1], 63 nM [1], 63 nM [1], 63 nM [1], 63 nM [1] |
In vitro |
GW842166X shows similar potency and efficacy for rat and human recombinant CB2 receptors with EC50 of 91 nM and 63nM, respectively., [1] GW-842166X exhibits full agonist potency with an EC50 of 133 nM and Emax of 101% in cyclase assays. GW-842166X exhibits weak agonist potency with an EC50 of 7.780 uM and Emax of 84% in FLIPR assays. [2] |
In vivo |
GW842166X has an oral bioavailability of 58% and a half-life of 3 h when dosed orally in the rat. GW842166X has extremely high potency with an oral ED50 of 0.1 mg/kg and shows full reversal of hyperalgesia at 0.3 mg/kg in the FCAa model of inflammatory pain. [1] GW842166X orally administrated at a dose of 15 mg/kg for 8 days produced a significant reversal of the CCI induced decrease in paw withdrawal threshold in a rat model of neuropathic pain. [3] |
Kinase Assay |
Determination of cannabinoid CB2 Receptor Agonist Activity, GW842166X is prepared as 10 mM stocks in DMSO. EC50 values (the concentration required to produce 50% maximal response) are estimated using dilutions of between 3- and 5-fold into DMSO. GW842166X in DMSO (1% final assay volume) is transferred into black, clear bottom, microtitre plates from NUNC (96- or 384-well). Cells are suspended at a density of 0.2 OD100/ml in SC media lacking histidine, uracil, tryptophan, adenine and leucine and supplemented with 10 mM 3-aminotriazole, 0.1 M sodium phosphate pH 7.0, and 20 M fluorescein di-beta-D-glucopyranoside (FDGlu). This mixture (50 ul per well for 384-well plates, 200ul per well for 96-well plates) is added to agonist in the assay plates. After incubation at 30 C for 24 hours, fluorescence resulting from degradation of FDGlu to fluorescein due to exoglucanase, an endogenous yeast enzyme produced during agonist-stimulated cell growth, is determined using a Spectrofluor microtitre plate reader (excitation wavelength: 485nm, emission wavelength: 535nm). Fluorescence is plotted against compound concentration and iteratively curve fitted using a four parameter fit to generate a concentration effect value. |
Molecular Weight (MW) |
449, 25 |
Picture ChemicalStructure Description |
GW842166X Chemical Structure |
Solubility (25C) |
DMSO 20 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL |
Storage |
2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO |
Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.
All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.