化学信息:
化学名
|
1-phenyl-3-[4-(phenylsulfamoyl)phenyl]thiourea
|
|
简称
|
LED209
|
别名
|
LED 209, LED-209
|
中文名
|
N/A
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化学式
|
C19H17N3O2S2
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分子量
|
383.49
|
CAS号
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245342-14-7
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纯度
|
98%
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溶剂/溶解度
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Water<1mg/ml; DMSO20mg/ml; Ethanol20mg/ml
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溶液配制
|
5mg加入1.3ml DMSO,或者每3.83mg加入1ml DMSO,配制成10mM溶液。SC3310-10mM用DMSO配制。
|
生物信息:
产品描述
|
LED209 is a potent small molecule inhibitor of bacterial receptor QseC, is a potent prodrug that is highly selective for QseC.
|
信号通路
|
Anti-infection
|
靶点
|
Antibacterial
|
-
|
-
|
-
|
-
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IC50
|
-
|
-
|
-
|
-
|
-
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体外研究
|
LED209 has desirable pharmacokinetics and does not present toxicity in vitro and in rodents. This is a unique antivirulence approach, with a proven broad-spectrum activity against multiple Gram-negative pathogens that cause mammalian infections.The LED209 QseC inhibitor has a unique mode of action by acting as a prodrug scaffold to deliver a warhead that allosterically modifies QseC, impeding virulence in several Gram-negative pathogens. LED209 is QseC sensor kinase inhibitor , as a potential lead compound to combat infections with Legionella or Mycobacterium spp. LED209 inhibits the binding of signals to QseC, preventing its autophosphorylation and consequently inhibiting QseC-mediated activation of virulence gene expression. LED209 inhibits EHEC virulence traits in vitro. LED209 markedly inhibits the virulence of several pathogens in animals. Inhibition of signaling offers a strategy for the development of broad-spectrum antimicrobial drugs.
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体内研究
|
N/A
|
临床实验
|
N/A
|
特征
|
N/A
|
相关实验数据(此数据来自于公开文献,碧云天并不保证其有效性):
酶活性检测实验
|
方法
|
N/A
|
细胞实验
|
细胞系
|
N/A
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浓度
|
N/A
|
处理时间
|
N/A
|
方法
|
N/A
|
动物实验
|
动物模型
|
N/A
|
配制
|
N/A
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剂量
|
N/A
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给药方式
|
N/A
|
参考文献:
1. CurtismM, et al. MBio. 2014 Nov 11, 5(6), e02165.
2. Harrison CF, et al. Microbiology. 2015 Jul, 161(7), 1392-406.
3. Rasko DA, et al. Science. 2008 Aug 22, 321(5892), 1078-80.
包装清单:
产品编号
|
产品名称
|
包装
|
SC3310-10mM
|
LED209 (QseC抑制剂)
|
10mM×0.2ml
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SC3310-5mg
|
LED209 (QseC抑制剂)
|
5mg
|
SC3310-25mg
|
LED209 (QseC抑制剂)
|
25mg
|
—
|
说明书
|
1份
|
保存条件:
-20℃保存,至少一年有效。5mg和25mg包装也可室温保存,至少6个月有效。如果溶于非DMSO溶剂,建议分装后-80℃保存,预计6个月内有效。
注意事项:
本产品仅限于专业人员的科学研究用,不得用于临床诊断或治疗,不得用于食品或药品,不得存放于普通住宅内。
为了您的安全和健康,请穿实验服并戴一次性手套操作。