RS102895盐酸盐
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- CAS号:
- 1173022-16-6
- 英文名:
- RS-102895 hydrochloride
- 英文别名:
- 3-trihydroxybenzene;RS-102895;RS 102895;RS102895;1'-(4-(Trifluoromethyl)phenethyl)spiro[benzo[d][1,3]oxazine-4,4'-piperidin]-2(1H)-one hydrochloride;Spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one, 1'-[2-[4-(trifluoromethyl)phenyl]ethyl]-, hydrochloride;Spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one, 1'-[2-[4-(trifluoromethyl)phenyl]ethyl]-, hydrochloride (1:1)
- 中文名:
- RS102895盐酸盐
- 中文别名:
- 1'-(4-三氟甲基苯乙基)螺[苯并[D][1,3]噁嗪-4,4'-哌啶]-2(1H)-酮盐酸盐;1'-(4-三氟甲基苯乙基)螺[苯并[D][1,3]噁嗪-4,4'-哌啶]-2(1H)-酮盐酸盐;1'-(4-(三氟甲基)苯乙基)螺[苯并[D][1,3]恶嗪-4,4'-哌啶]-2(1H)-酮 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 盐酸盐
- CBNumber:
- CB52729375
- 分子式:
- C21H22ClF3N2O2
- 分子量:
- 426.86
- MOL File:
- 1173022-16-6.mol
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RS102895盐酸盐化学性质
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储存条件:
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Inert atmosphere,Room Temperature
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溶解度:
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DMF: 25 mg/ml; DMSO: 30 mg/ml; DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml; Ethanol: 2 mg/ml
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形态:
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Powder
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颜色:
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White to off-white
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RS102895盐酸盐性质、用途与生产工艺
RS102895 hydrochloride 是一种有效的 CCR2 拮抗剂，IC50 值为 360 nM，对 CCR1 无作用。
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CCR2
360 nM (IC
50
)
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CCR1
17800 nM (IC
50
)
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Human α
1a
receptor
130 nM (IC
50
)
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Human α
1d
receptor
320 nM (IC
50
)
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5HT-1a receptor
470 nM (IC
50
)
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RS102895 hydrochloride 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.
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.
RS102895盐酸盐
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| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | S7538 | RS102895盐酸盐
RS-102895 Hydrochloride | 1173022-16-6 | 5mg | 1203.93元 |
| 2024/04/30 | S7538 | RS102895盐酸盐
RS-102895 Hydrochloride | 1173022-16-6 | 25mg | 3595.41元 |
1173022-16-6, RS102895盐酸盐 相关搜索:
- 药靶配体
- 新型抑制剂
- 1'-(4-三氟甲基苯乙基)螺[苯并[D][1,3]噁嗪-4,4'-哌啶]-2(1H)-酮盐酸盐
- 1'-(4-(三氟甲基)苯乙基)螺[苯并[D][1,3]恶嗪-4,4'-哌啶]-2(1H)-酮 盐酸盐
- 1'-(4-三氟甲基苯乙基)螺[苯并[D][1,3]噁嗪-4,4'-哌啶]-2(1H)-酮盐酸盐
- 1'-(4-(三氟甲基)苯乙基)螺[苯并[D][1,3]恶嗪-4,4'-哌啶]-2(1H)-酮 盐酸盐
- 1173022-16-6
- 1'-(4-(Trifluoromethyl)phenethyl)spiro[benzo[d][1,3]oxazine-4,4'-piperidin]-2(1H)-one hydrochloride
- RS-102895;RS 102895;RS102895
- Spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one, 1'-[2-[4-(trifluoromethyl)phenyl]ethyl]-, hydrochloride (1:1)
- 3-trihydroxybenzene
- Spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one, 1'-[2-[4-(trifluoromethyl)phenyl]ethyl]-, hydrochloride