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162112-37-0

中文名稱 RWJ 50271
英文名稱 RWJ 50271
CAS 162112-37-0
分子式 C18H17F3N4O2S
分子量 410.41
MOL 文件 162112-37-0.mol
更新日期 2024/12/15 19:35:18
162112-37-0 結(jié)構(gòu)式 162112-37-0 結(jié)構(gòu)式

基本信息

中文別名
化合物RWJ 50271
英文別名
RWJ 50271
N-(3-hydroxypropyl)-5-methyl-1-[4-[3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]pyrazole-4-carboxamide
1H-Pyrazole-4-carboxamide, N-(3-hydroxypropyl)-5-methyl-1-[4-[3-(trifluoromethyl)phenyl]-2-thiazolyl]-
N-(3-Hydroxypropyl)-5-methyl-1-[-4-[3-(trifluoromethyl)phenyl)]-2-thiazolyl]-1H-pyrazole-4-carboxamide

物理化學(xué)性質(zhì)

密度1.44±0.1 g/cm3(Predicted)
儲(chǔ)存條件Store at RT
溶解度<41.04mg/ml in DMSO
酸度系數(shù)(pKa)14.28±0.46(Predicted)
形態(tài)Solid
顏色White to off-white

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H315-H319

常見問題列表

生物活性
RWJ 50271 是一種選擇性的,具有口服活性的 LFA-1/ICAM-1 相互作用抑制劑,IC50 值為 5.0 μM (HL60 cells)。RWJ 50271 抑制 LFA-1/ICAM-1 介導(dǎo)的細(xì)胞粘附。
靶點(diǎn)

IC50: 5.0 μM (LFA-1/ICAM-1, HL60 cells)

體外研究

RWJ 50271 inhibits adhesion of peripheral blood lymphocytes to plastic immobilized SICAM-1.
RWJ 50271 inhibits both human and murine NK activity (IC 50 =5.0 μM) in an LFA-1/ICAM-1-dependent natural killer [NK] cytotoxicity assay.
RWJ 50271 does not inhibit Mac-1/ICAM-1, E-selectidsialyl Lewis X or VLA-4/VCAM-1-mediated cell adhesion up to 20 μM concentrations.
RWJ 50271 does not alter the LFA-1 expression levels on HL60 cells.
RWJ 50271 inhibits adhesion of peripheral blood lymphocytes to plastic immobilized SICAM-1.
RWJ 50271 does not exhibit any toxic activity up to 100 μM concentrations.

體內(nèi)研究

RWJ 50271 (50 mg/kg; p.o.) is effective in animal model of inflammation.

Animal Model: Mice, the delayed-type hypersensitivity [DTH] reaction model
Dosage: 50 mg/kg
Administration: Oral administration
Result: Significantly reduced foot pad swelling (>50%) 48 h after the challenge.
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