| CAS NO: | 666260-75-9 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 449.25 |
|---|---|
| Formula | C18H17Cl2F3N4O2 |
| CAS No. | 666260-75-9 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 20 mg/mL (44.5 mM) |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| Solubility (In vivo) | 30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL |
| Technical info | Synonym: GW-842166X; GW842166; GW 842166X; 842166X; 842166; GW-842166; GW842166X; GW 842166 Chemical Name: 2-((2,4-dichlorophenyl)amino)-N-((tetrahydro-2H-pyran-4-yl)methyl)-4-(trifluoromethyl)pyrimidine-5-carboxamide InChi Key: TWQYWUXBZHPIIV-UHFFFAOYSA-N InChi Code: 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) SMILES Code: O=C(C1=CN=C(NC2=CC=C(Cl)C=C2Cl)N=C1C(F)(F)F)NCC3CCOCC3 |
| In Vitro | In vitro activity: GW842166X shows similar potency and efficacy for rat and human recombinant CB2 receptors with EC50 of 91 nM and 63nM, respectively. 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 μM and Emax of 84% in FLIPR assays. |
|---|---|
| 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. 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. |
| Animal model | Rat model of neuropathic pain |
| Formulation & Dosage | Dissolved in saline; 15 mg/kg; p.o. administration once daily for 8 days |
| References | J Med Chem. 2007 May 31;50(11):2597-600; Br J Pharmacol. 2008 Jan;153(2):390-401 |
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