RS 102895
RS 102895(RS 102895)
CAS: 300815-41-2
化学式: C21H21F3N2O2
| 中文名 | RS 102895 |
| 英文名 | RS 102895 |
| 别名 | 化合物RS102895 RS 102895 盐酸盐 1'-(4-(三氟甲基)苯乙基)螺[苯并[D][1,3]恶嗪-4,4'-哌啶]-2(1H)-酮 1'-[2-[4-(三氟甲基)苯基]乙基]-螺[4H-3,1-苯并恶嗪-4,4'-哌啶]-2(1H)-酮 1'-[2-[4-(三氟甲基)苯基]乙基]-螺[4H-3,1-苯并恶嗪-4,4'-哌啶]-2(1H)-酮盐酸盐 1'-[2-[4-(三氟甲基)苯基]乙基]-螺[4H-3,1-苯并噁嗪-4,4'-哌啶]-2(1H)-酮盐酸盐 |
| 英文别名 | RS 102895 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 |
| CAS | 300815-41-2 |
| 化学式 | C21H21F3N2O2 |
| 分子量 | 390.4 |
| 密度 | 1.33±0.1 g/cm3 (20 ºC 760 Torr) |
| 沸点 | 446.1±45.0 °C(Predicted) |
| 溶解度 | DMSO: 18mg/ml，澄清，无色 |
| 酸度系数 | 13.46±0.20(Predicted) |
| 存储条件 | Desiccate at RT |
| 外观 | 粉末 |
| 颜色 | white |
| 体外研究 | RS102895 is a potent CCR2 antagonist, with an IC 50 of 360 nM, and shows no effect on CCR1. RS102895 also inhibits human α1a and α1d receptors, rat brain cortex 5HT1a receptor in cells with IC 50 s of 130, 320, 470 nM, respectively. RS102895 suppresses wild type and D284N mutant MCP-1 receptor (IC 50 , 550 nM and 568 nM, respectively), less potently inhibits D284A MCP-1 receptor (IC 50 , 1892 nM), and has no effects on E291A, E291Q, D284A/E291A or D284N/E291Q (IC 50 , >100,000 nM). RS102895 ameliorates the increased extracellular matrix (ECM) protein expression by inhibition of CCR2 at 10 μM, and obviously blocks fibronectin and type IV collagen protein expression in high glucose (HG)-stimulated mesangial cells (MCs) at 1 or 10 μM. RS102895 (10 μM) also abrogates the increased TGF-1 levels in MCs treated with MCP-1. |
| 体内研究 | 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. |
| 安全术语 | S22 - 切勿吸入粉尘。 S24/25 - 避免与皮肤和眼睛接触。 |
| WGK Germany | 3 |
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