300815-41-2

中文名称 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

英文名称 RS 102895

CAS 300815-41-2

分子式 C21H21F3N2O2

分子量 390.4

MOL 文件 300815-41-2.mol

更新日期 2024/06/03 14:41:43

300815-41-2 结构式

基本信息物理化学性质安全数据常见问题列表

基本信息

中文别名

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 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

所属类别

生物化工：激动剂抑制剂

物理化学性质

沸点446.1±45.0 °C(Predicted)

密度1.33±0.1 g/cm3 (20 ºC 760 Torr)

储存条件Desiccate at RT

溶解度DMSO: 18 mg/mL, clear, colorless

酸度系数(pKa)13.46±0.20(Predicted)

形态powder

颜色白色

安全数据

安全说明22-24/25

WGK Germany3

常见问题列表

生物活性

RS102895 是一种有效的 CCR2 拮抗剂，IC50 值为 360 nM，对 CCR1 无作用。

靶点

CCR2

360 nM (IC ₅₀ )

CCR1

17800 nM (IC ₅₀ )

Human α _1a receptor

130 nM (IC ₅₀ )

Human α _1d receptor

320 nM (IC ₅₀ )

5HT-1a receptor

470 nM (IC ₅₀ )

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.