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300816-15-3

中文名稱 6 - 甲基-1,1' - [2 - (5 - 甲基- 2-苯基- 4-惡唑基)乙基] - 螺[4H - 3-1,1 - 苯并惡嗪- 4,4' -哌啶]-2(1H)-酮
英文名稱 RS 504393
CAS 300816-15-3
分子式 C25H27N3O3
分子量 417.5
MOL 文件 300816-15-3.mol
更新日期 2024/12/26 10:13:45
300816-15-3 結(jié)構(gòu)式 300816-15-3 結(jié)構(gòu)式

基本信息

中文別名
化合物RS 504393
6-甲基-1'-[2-(5-甲基-2-苯基-4-惡唑基)乙基]螺[4H-3,1-苯并惡嗪-4,4'-哌啶]-2(1H)-酮
6-甲基-1'-(2-(5-甲基-2-苯基惡唑-4-基)乙基)螺[苯并[D][1,3]惡嗪-4,4'-哌啶]-2(1H)-酮
6-甲基-1'-[2-(5-甲基-2-苯基-噁唑-4-基)乙基]-螺[4H-3,1-苯并噁嗪-4,4'-哌啶]-2(1H)-酮
6 - 甲基-1,1' - [2 - (5 - 甲基- 2-苯基- 4-惡唑基)乙基] - 螺[4H - 3-1,1 - 苯并惡嗪- 4,4' -哌啶]-2(1H)-酮
英文別名
RS 504393
RS-504393
RS504393
RS504393 >=98% (HPLC)
6-Methyl-1'-[2-(5-Methyl-2-phenyl-4-oxazolyl)ethyl]-spiro[4H-3,1-benzoxazine-4,4'-piperidi
6-Methyl-1'-(2-(5-methyl-2-phenyloxazol-4-yl)ethyl)spiro-[benzo[d][1,3]oxazine-4,4'-piperidin]
6-Methyl-1'-(2-(5-methyl-2-phenyloxazol-4-yl)ethyl)spiro-[benzo[d][1,3]oxazine-4,4'-piperidin]-2(
6-Methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]-spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one
6-Methyl-1'-(2-(5-Methyl-2-phenyloxazol-4-yl)ethyl)spiro[benzo[d][1,3]oxazine-4,4'-piperidin]-2(1H)-one
Spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one, 6-Methyl-1'-[2-(5-Methyl-2-phenyl-4-oxazolyl)ethyl]-

物理化學(xué)性質(zhì)

密度1.28
儲存條件2-8°C
溶解度DMSO:可溶1mg/mL,澄清(加熱)
形態(tài)粉末
顏色白色至米色

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H315-H319-H335
危險品標志Xi
危險類別碼36/37/38
安全說明26
WGK Germany3

常見問題列表

生物活性
RS 504393 是一種選擇性的 CCR2 拮抗劑,作用于人重組 CCR2 和 CCR1 受體,IC50 值分別為 89 nM 和 > 100 μM。
靶點

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 )

體外研究

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.

體內(nèi)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.

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