6 - 甲基-1,1' - [2 - (5 - 甲基- 2-苯基- 4-恶唑基)乙基] - 螺[4H - 3-1,1 - 苯并恶嗪- 4,4' -哌啶]-2(1H)-酮
- CAS号:300816-15-3
- 英文名:RS 504393
- 中文名:6 - 甲基-1,1' - [2 - (5 - 甲基- 2-苯基- 4-恶唑基)乙基] - 螺[4H - 3-1,1 - 苯并恶嗪- 4,4' -哌啶]-2(1H)-酮
- CBNumber:CB5837883
- 分子式:C25H27N3O3
- 分子量:417.5
- MOL File:300816-15-3.mol
- 密度 :1.28
- 储存条件 :2-8°C
- 溶解度 :DMSO: soluble1mg/mL, clear (warmed)
- 形态 :powder
- 颜色 :white to beige
6 - 甲基-1,1' - [2 - (5 - 甲基- 2-苯基- 4-恶唑基)乙基] - 螺[4H - 3-1,1 - 苯并恶嗪- 4,4' -哌啶]-2(1H)-酮性质、用途与生产工艺
- 生物活性 RS 504393 是一种选择性的 CCR2 拮抗剂,作用于人重组 CCR2 和 CCR1 受体,IC50 值分别为 89 nM 和 > 100 μM。
-
靶点
CCR2
89 nM (IC 50 )
Human α 1a receptor
72 nM (IC 50 )
Human α 1d receptor
460 nM (IC 50 )
5HT-1a receptor
1070 nM (IC 50 )
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体外研究
RS 504393 inhibits the MCP-1-induced chemotaxis with an IC 50 of 330 nM. RS 504393 treatment suppresses allergen induced β-hexosaminidase release significantly. Without allergen priming, MCP-1 induces mast cell degranulation, which is completely suppressed by RS 504393.
-
体内研究
RS504393 (0.3-3 μg) with CCL2 progressively blocks thermal hyperalgesia dose-dependently in mice. RS 504393 (5 mg/kg, i.v.) supresses the elevated numbers of leukocytes and increased total protein content in BALF induced by The LPS. RS504393 significantly down regulates the LPS-induced elevation of IL-1β, PAI-1 mRNA and protein expressions. RS504393 significantly suppresses induced lung edema, protein-rich fluid, polymorphonuclear accumulation and bronchial wall thickening induced by LPS. RS-504393 significantly reduces renal pathology, especially the extensive interstitial fibrosis mediated by decrease in type I collagen synthesis in a UUO model.
- 更新日期:2024/11/08
- 产品编号:HY-15418
- 产品名称:RS 504393
- CAS编号:
- 包装:1 mg
- 价格:324元
- 更新日期:2024/11/08
- 产品编号:HY-15418
- 产品名称:6 - 甲基-1,1' - [2 - (5 - 甲基- 2-苯基- 4-恶唑基)乙基] - 螺[4H - 3-1,1 - 苯并恶嗪- 4,4' -哌啶]-2(1H)-酮 RS 504393
- CAS编号:300816-15-3
- 包装:5mg
- 价格:810元
- 公司名称:CHEMSWORTH
- 联系电话:--
- 电子邮件:info@chemsworth.com
- 国家:印度
- 产品数:6700
- 优势度:30