474960-44-6
中文名稱
2-溴-N-[4-氯-3-[[(3R)-1-甲基-3-吡咯烷基]氧基]苯基]-4,5-二甲氧基-苯磺酰胺
英文名稱
2-Bromo-N-[4-chloro-3-[[(3R)-1-methyl-3-pyrrolidinyl]oxy]phenyl]-4,5-dimethoxybenzenesulfonamide
CAS
474960-44-6
分子式
C19H22BrClN2O5S
分子量
505.81
MOL 文件
474960-44-6.mol
474960-44-6 結(jié)構(gòu)式
基本信息
中文別名
2-溴-N-[4-氯-3-[[(3R)-1-甲基-3-吡咯烷]氧基]苯基]-4,5-二甲氧基苯磺酰胺2-溴-N-[4-氯-3-[[(3R)-1-甲基-3-吡咯烷基]氧基]苯基]-4,5-二甲氧基-苯磺酰胺
英文別名
CS-1139SB 657510
2-Bromo-N-[4-chloro-3-[[(3R)-1-methyl-3-pyrrolidinyl]oxy]phenyl]-4,5-dimethoxybenzenesulfonamide
2-bromo-N-[4-chloro-3-[(3R)-1-methylpyrrolidin-3-yl]oxy-phenyl]-4,5-dimethoxy-benzenesulfonamide
BenzenesulfonaMide, 2-broMo-N-[4-chloro-3-[[(3R)-1-Methyl-3-pyrrolidinyl]oxy]phenyl]-4,5-diMethoxy-
常見問題列表
生物活性
SB-657510 是選擇性的 urotensin II (UII) receptor (UT) 拮抗劑。 對(duì)于人，猴，貓，大鼠和小鼠的受體的 Ki 值分別為 61、17、30、65 和 56 nM。SB-657510 通過抑制 UII 誘導(dǎo)的人類血管內(nèi)皮細(xì)胞中炎性介質(zhì)，如粘附分子，細(xì)胞因子和組織因子上調(diào)發(fā)揮抗炎作用。體外研究
SB-657510 dramatically blocks the UII-induced increase in adhesion between U937 and EA.hy926 cell. SB-657510 (1 μM; 0.5-8 hours) blocks the expression of tissue factor induced by UII in endothelial cells.
SB-706375 (1-10000 nM) inhibits [Ca
2+
]
i
mobilization elicited by 10?nM hU-II with an IC
50
of 180?nM.
Western Blot Analysis
| Cell Line: | EA.hy926 cells (UII-induced) |
| Concentration: | 1 μM |
| Incubation Time: | 0.5, 1, 2, 4, 8 hours |
| Result: | Remarkably decreased the UII-induced protein expression of tissue factor. |
體內(nèi)研究
SB-657510 inhibits the progression of high-fat diet induced atherosclerosis and diabetes-associated atherosclerosis.
Levels of phosphorylated ERK are significantly attenuated in the aorta of SB-657510-treated (30 mg/kg/day) diabetic mice (Male Apoe KO mice).