193551-21-2
193551-21-2 結(jié)構(gòu)式
基本信息
反式-1-(4-羥基環(huán)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]環(huán)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)環(huán)己醇
SB 239063
SB-239063
SB239063
SB 239063 - CAS 798558-40-4 - Calbiochem
rans-4-[4-(4-Fluorophenyl)-5-(2-methoxy-4-pyrimidinyl)-1H-imidazol-1-yl]cyclohexano
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-
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
制備方法
![Cyclohexanone, 4-[4-(4-fluorophenyl)-5-(2-methoxy-4-pyrimidinyl)-1H-imidazol-1-yl]-](/CAS/20210305/GIF/193551-20-1.gif)
193551-20-1
193551-21-2
以化合物（CAS: 193551-20-1）為起始原料，合成(1r,4r)-rel-4-(4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)-1H-咪唑-1-基)環(huán)己醇的一般步驟如下： 實(shí)施例2：反式-1-(4-羥基環(huán)己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑的合成 向?qū)嵤├?（j）中制備的化合物溶液（0.099 g，溶解于MeOH/THF（1 mL，體積比1:1）中，對(duì)應(yīng)0.27 mmol）加入NaBH4溶液（1 mL，1 M溶液。該NaBH4溶液通過(guò)將0.10 g NaBH4、MeOH（2.5 mL）和25% NaOMe的MeOH溶液（0.2 mL）混合制備而成）。反應(yīng)混合物攪拌10分鐘后，用飽和Na2CO3溶液淬滅反應(yīng)，隨后蒸發(fā)除去溶劑。殘余物通過(guò)從MeOH/H2O混合溶劑中重結(jié)晶純化，得到目標(biāo)產(chǎn)物(1r,4r)-rel-4-(4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)-1H-咪唑-1-基)環(huán)己醇，為白色針狀晶體（0.063 g，收率63%）。產(chǎn)物的熔點(diǎn)為188-190℃。
參考文獻(xiàn)：
[1] Patent: US6329526, 2001, B1
| 報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
| 2026/03/03 | S7741 | 反式-1-(4-羥基環(huán)己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑 SB239063 | 193551-21-2 | 5mg | 1115.26元 |
| 2026/03/03 | S7741 | 反式-1-(4-羥基環(huán)己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑 SB239063 | 193551-21-2 | 10mM (1mL in DMSO) | 1285.83元 |
| 2026/03/03 | S7741 | 反式-1-(4-羥基環(huán)己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑 SB239063 | 193551-21-2 | 25mg | 4083.98元 |
常見問(wèn)題列表
| Target | Value |
|
p38α
(Cell-free assay) | 44 nM |
|
p38β
(Cell-free assay) | 44 nM |
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. |
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. |