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LED209
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LED209图片
CAS NO:245342-14-7
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
LED209 是一种有效的细菌受体 QseC 小分子抑制剂,是一种有效的前药,对 QseC 具有高度选择性。
Cas No.245342-14-7
别名N-苯基-4-(3-苯基硫代脲基)苯磺酰胺
化学名(Z)-N'-phenyl-N-(4-(N-phenylsulfamoyl)phenyl)carbamimidothioic acid
Canonical SMILESO=S(C1=CC=C(N/C(S)=N/C2=CC=CC=C2)C=C1)(NC3=CC=CC=C3)=O
分子式C19H17N3O2S2
分子量383.49
溶解度<3.83 mg/mL in DMSO,<2.33 mg/mL in EtOH,<2.38 mg/mL in Water
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Description:

IC50:<10 μM

Many bacterial pathogens rely on a conserved membrane histidine sensor kinase, QseC, to respond to host adrenergic signaling molecules and bacterial signals in order to promote the expression of virulence factors. LED209 is a potent prodrug that is highly selective for QseC.

In vitro: LED209-mediated inhibition of virulence gene expression inhibited the secretion of EspA and EspB, two proteins encoded within the locus of enterocyte effacement that are required for Escherichia coli (EHEC) to translocate bacterial proteins into host cells and cause attaching-effacing (AE) lesions. At 5 pM, LED209 abolished EHEC AE lesion formation on cultured epithelial cells. Unlike conventional antibiotics, LED209 does not kill or hinder EHEC growth or trigger the EHEC SOS response [1].

In vivo: LED209 [20 mg per kilogram of body weight (mg/kg)] was given orally to mice 3 hours before and 3 hours after intraperitoneal injection of a lethal dose of S. typhimurium. Twenty-four hours after infection, only 30% of untreated mice remained alive, whereas 80% of the LED209-treated mice were still alive. All the S. typhimurium– infected mice died within 72 hours of infection, and 20% of LED209-treated mice survived up to 12 days [1].

Clinical trial: Up to now, LED209 is still in the preclinical development stage.

Reference:
[1] Rasko DA, Moreira CG, Li de R, Reading NC, Ritchie JM, Waldor MK, Williams N, Taussig R, Wei S, Roth M, Hughes DT, Huntley JF, Fina MW, Falck JR, Sperandio V.  Targeting QseC signaling and virulence for antibiotic development. Science. 2008 Aug 22;321(5892):1078-80.