中文名 | SB 239063 |
英文名 | SB 239063 |
别名 | 化合物L-779450 反式-1-(4-羟基环己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑 反-4-[4-(4-氟苯基)-5-(2-甲氧基-4-嘧啶基)-1H-咪唑-1-基]环己醇 (1R,4R)-REL-4-(4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)-1H-咪唑-1-基)环己醇 |
英文别名 | CS-402 SB 239063 TRANS-1-(4-HYDROXYCYCLOHEXYL)-4-(FLUOROPHENYL)-5-(2-METHOXYPYRIMIDIN-4-YL) IMIDAZOLE TRANS-4-[4-(4-FLUOROPHENYL)-5-(2-METHOXY-4-PYRIMIDINYL)-1H-IMIDAZOL-1-YL]CYCLOHEXANOL TRANS-1-(4-HYDROXYCYCLOHEXYL)-4-(4-FLUOROPHENYL)-5-(2-METHOXYPYRIMIDIN-4-YL) IMIDAZOLE TRANS-1-(4-HYDROXYCYCLOHEXYL)-4-(4-FLUOROPHENYL)-5-(2-METHOXYPYRIDIMIDIN-4-YL)IMIDAZOLE Cyclohexanol, 4-[4-(4-fluorophenyl)-5-(2-methoxy-4-pyrimidinyl)-1H-imidazol-1-yl]-, trans- |
CAS | 193551-21-2 |
化学式 | C20H21FN4O2 |
分子量 | 368.4 |
InChIKey | ZQUSFAUAYSEREK-WKILWMFISA-N |
熔点 | 206-207.2°C |
溶解度 | DMSO: 11 mg/mL |
存储条件 | 2-8°C |
外观 | 白色固体 |
颜色 | white |
体外研究 | SB 239063 (0.1–10 μM ; 29 hours, 47 hours) increases apoptosis of eosinophils in a dose-related in the presence of 10 pM IL-5 at every time point from 21 hours onwards. SB 239063 potently inhibits IL-1 and TNF- a production in LPS-stimulated human peripheral blood monocytes with IC 50 values of 120 nM and 350 nM, respectively. Apoptosis Analysis Cell Line: Eosinophils (guinea pig BALs) Concentration: 0.1μM, 1μM, 10μM Incubation Time: 29 hours, 47 hours Result: Increased apoptosis of eosinophils in a dose-related in the presence of 10 pM IL-5 at every time point from 21 hours onwards. |
体内研究 | SB 239063 (12 mg/kg; p.o.; 1 hour before and 4 hours after OA challenge; b.i.d. for 3 days) significantly inhibits the resultant antigen-induced airway eosinophilia. SB 239063 (12 mg/kg; p.o.) almost abolishes ovalbumin (OA)-induced airway eosinophilia (~ 93% inhibition) by inhalation. SB 239063 is a potent inhibitor of LPS-induced TNF-alpha production in the mouse peritoneal cavity with an EC 50 of 5.8 mg/kg (2.8–10.3; 95% CL). Animal Model: Male BALB/c mice (18–20 g) Dosage: 12 mg/kg Administration: Oral administration; 1 h before and 4 h after OA challenge; bis in die for 3 days Result: Significantly inhibited the resultant antigen-induced airway eosinophilia. |
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 |
RTECS | GV9458000 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.714 ml | 13.572 ml | 27.144 ml |
5 mM | 0.543 ml | 2.714 ml | 5.429 ml |
10 mM | 0.271 ml | 1.357 ml | 2.714 ml |
5 mM | 0.054 ml | 0.271 ml | 0.543 ml |
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