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KM11060,≥99% (HPLC)

别名:7-氯-4-(4-((4-氯苯基)磺酰基)-1-哌嗪基)喹啉;7-CHLORO-4-(4-(4-CHLOROPHENYLSULFONYL)PIPERAZIN-1-YL)QUINOLINE;7-CHLORO-4-[4-[4-CHLOROPHENYL)SULFONYL]-1-PIPERAZINYL]QUINOLINE

CAS:774549-97-2;分子式:C19H17Cl2N2O2S;分子量:422.33
制造商品牌: BSZH 科学公司
货号(SKU): K06156
CAS号: 774549-97-2
MDL号: MFCD01524977
增值税发票 √ 免费送货 √ 订货电话:010-68689484
¥755.00

产品描述

本品可溶于DMSO

General description

一种F508del-CFTR校正剂。

KM11060 is a novel corrector of the F508del-CFTR trafficking defect. Target: CFTR in vitro: Small-molecule correctors such as KM11060 may serve as useful pharmacological tools in studies of the F508del-CFTR processing defect and in the development of cystic fibrosis therapeutics. KM11060 rescues F508del-CFTR trafficking in cultured cells and native epithelial tissues. KM11060 partially corrects F508del-CFTR processing and increases surface expression to 75% of that observed in cells incubated at low temperature. Up to 50% of the F508del-CFTR in cells treated with KM11060 was complex-glycosylated, indicating passage through the Golgi. KM11060 as a promising compound for further development of CF therapeutics.
In vivo: In LPS-induced acute lung inflammation, blockade of PSGL-1 (P-selectin glycoprotein ligand-1) or P-selectin, antagonism of PAF by WEB2086, or correction of mutated CFTR trafficking by KM11060 could significantly increase plasma lipoxin A4 levels in F508del relevant to wildtype mice.

KM11060是F508del-CFTR交易缺陷的新型校正器。目标:体外CFTR:KM11060等小分子校正剂可作为F508del-CFTR加工缺陷研究和囊性纤维化治疗药物开发中的有用药理工具。 KM11060挽救了F508del-CFTR在培养细胞和天然上皮组织中的运输。 KM11060部分纠正F508del-CFTR加工,并将表面表达提高到在低温下孵育的细胞中观察到的表面表达的75%。用KM11060处理的细胞中,高达50%的F508del-CFTR被复合糖基化,表明其通过了高尔基体。 KM11060是用于CF治疗药物的有前途的化合物。
体内:在LPS诱导的急性肺部炎症中,对PSGL-1(P-选择素糖蛋白配体-1)或P-选择素的阻滞,WEB2086对PAF的拮抗作用或KM11060对CFTR突变运输的纠正可显着增加血浆脂蛋白A4与野生型小鼠有关的F508del中的水平。


安全信息

风险声明 (欧洲) 23/24/25
安全声明 (欧洲) 26-36
WGK德国 WGK 3
商品规格
属性名称属性值
储存温度 Storage temp.-20°C低温冷冻
全球实时库存 Availability √美国St. Louis ≥ 33 | 欧洲Eur. ≥ 27 | 東京Tokyo ≥ 9 | 香港与北京 ≥ 16