| Identification | Back Directory | [Name]
RS 102895 | [CAS]
300815-41-2 | [Synonyms]
RS 102895 HYDROCHLORIDE
1'-(4-(trifluoromethyl)phenethyl)spiro[benzo[d][1,3]oxazine-4,4'-piperidin]-2(1H)-one
1'-[2-[4-(trifluoromethyl)phenyl]ethyl]-spiro[4h-3,1-benzoxazine-4,4'-peperidin]-2(1h)-one
Spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one, 1'-[2-[4-(trifluoromethyl)phenyl]ethyl]-
1'-(4-(TrifluoroMethyl)phenethyl)spiro[benzo[d][1,3]oxazine-4,4'-piperidin]-2(1H)-one hydrochloride
1'-[2-[4-(trifluoromethyl)phenyl]ethyl]spiro[1H-3,1-benzoxazine-4,4'-piperidine]-2-one,hydrochloride
1'-[2-[4-(TRIFLUOROMETHYL)PHENYL]ETHYL]-SPIRO[4H-3,1-BENZOXAZINE-4,4'-PIPERIDIN]-2(1H)-ONE HYDROCHLORIDE | [Molecular Formula]
C21H21F3N2O2 | [MDL Number]
MFCD08703093 | [MOL File]
300815-41-2.mol | [Molecular Weight]
390.4 |
| Chemical Properties | Back Directory | [Boiling point ]
446.1±45.0 °C(Predicted) | [density ]
1.33±0.1 g/cm3 (20 ºC 760 Torr) | [storage temp. ]
Desiccate at RT | [solubility ]
DMSO: 18 mg/mL, clear, colorless
| [form ]
powder
| [pka]
13.46±0.20(Predicted) | [color ]
white |
| Hazard Information | Back Directory | [Uses]
RS 102895 is a CCR2-selective chemokine receptor inhibitor. | [Biological Activity]
CCR2-selective chemokine receptor antagonist (IC 50 values are 0.36 and 17.8 μ M for inhibition of human recombinant CCR2b and CCR1 receptors respectively). Blocks MCP-1-stimulated calcium influx and chemotaxis with IC 50 values of 32 nM and 1.7 μ M respectively. Also inhibits α 1A , α 1D and 5-HT 1A receptors. | [in vivo]
RS102895 (3 g/L) causes progressive decrease in pain threshold in rats with bone cancer pain (BCP) at day 3-9 after surgery via intrathecal injection, but the pain threshold increases after 12 days. RS102895 also potently reverses the pattern of NR2B, nNOS, and SIGIRR expression in spinal cord[3]. | [IC 50]
CCR2: 360 nM (IC50); CCR1: 17800 nM (IC50); Human α1a receptor: 130 nM (IC50); Human α1d receptor: 320 nM (IC50); 5HT-1a receptor: 470 nM (IC50) |
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