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GW 842166X (CAS 666260-75-9) LS-H47

CB2 receptor agonist
LS-H47-1 / 1 mg / $175
LS-H47-5 / 5 mg / $215
LS-H47-10 / 10 mg / $255
LS-H47-25 / 25 mg / $345
USA Shipment Only
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Description: The peripheral cannabinoid (CB2) receptor is a G protein-coupled receptor (GPCR) that is localized predominantly in immune cells, monocytes, macrophages, and in several peripheral organs and binds the active component of cannabis, Δ9-tetrahydrocannabinol, as well as anandamide, an endogenous CB receptor ligand. GW 842166X is a peripheral cannabinoid (CB2) receptor agonist with ED50 values of 91 and 63 nM in rat and human, respectively. When administered orally to rats in the Freund's complete adjuvant (FCA) model of inflammatory pain, GW 842166X is highly potent with an ED50 value of 0.1 mg/kg and full reversal of hyperalgesia at 0.3 mg/kg. H47_ChemicalStructureImage.png
2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro-2H-pyran-4-yl)methyl]-4-(trifluoromethyl)-5-pyrimidinecarboxamide
 
biochemical, chemical, agonist
LS-H47
666260-75-9
C18H17Cl2F3N4O2
≥98%
A crystalline solid
0
Clc1ccc(Nc2ncc(C(=O)NCC3CCOCC3)c(n2)C(F)(F)F)c(Cl)c1
InChI=1S/C18H17Cl2F3N4O2/c19-11-1-2-14(13(20)7-11)26-17-25-9-12(15(27-17)18(21,22)23)16(28)24-8-10-3-5-29-6-4-10/h1-2,7,9-10H,3-6,8H2,(H,24,28)(H,25,26,27)
TWQYWUXBZHPIIV-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: CNR2 / CB2 related products

Usage Information

GW 842166X is supplied as a crystalline solid. A stock solution may be made by dissolving the GW 842166X in an organic solvent purged with an inert gas. GW 842166X is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF). The solubility of GW 842166X in ethanol is approximately 0.3 mg/ml and approximately 10 mg/ml in DMSO and DMF. GW 842166X is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, GW 842166X should first be dissolved in DMF and then diluted with the aqueous buffer of choice. GW 842166X has a solubility of approximately 0.25 mg/ml in a 1:3 solution of DMF:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Khanolkar, A.D., Lu, D., Ibrahim, M., et al. Cannabilactones: A novel class of CB2 selective agonists with peripheral analgesic activity. J. Med. Chem. 50, 6493-6500 (2007).
  2. Giblin, G.M.P., O’Shaughnessy, C.T., Naylor, A., et al. Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)-5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain. J. Med. Chem. 50(11), 2597-2600 (2007).

 


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