2. Metabolic Enzyme/Protease NF-κB MAPK/ERK Pathway Anti-infection
  3. Elastase NF-κB p38 MAPK Bacterial
  4. LasB-IN-1

LasB-IN-1 (compound 5f) 是高效且口服有效的 LasB 抑制剂 (IC50 = 8.7 μM)。LasB-IN-1 可有效抑制铜绿假单胞菌产生弹性蛋白酶和形成生物膜，同时通过下调 MAPK 和 NF-κB 通路减轻炎症反应。LasB-IN-1有可能成为一种新的抗耐药感染的候选用剂。

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LasB-IN-1 Chemical Structure

LasB-IN-1 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

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LasB-IN-1 相关抗体

Top Publications Citing Use of Products

查看 NF-κB 亚型特异性产品:

查看所有亚型
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 p38 MAPK 亚型特异性产品:

查看所有亚型
p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LasB-IN-1 (compound 5f) is a potent and orally active inhibitor of LasB (IC50 = 8.7 μM). LasB-IN-1 effectively attenuates elastase production and biofilm formation by P. aeruginosa while alleviating the inflammatory response through downregulating MAPK and NF-κB pathways. LasB-IN-1 is potential to be a novel anti-infective candidate against drug-resistant infections[1].

IC50 & Target

IC50: 8.7 μM (LasB)[1]
体外研究
(In Vitro)

LasB-IN-1 (5-10 μM, 10 h) 剂量依赖性地抑制铜绿假单胞菌 PAO1 株中 LasB (IC50 = 8.7 μM) 的表达、弹性酶的生物合成 (IC50 = 7.3 μM) 和生物膜的形成 (IC50 = 7.4 μM) [1]。
LasB-IN-1 (1.25-20 μM, 24 h) 对 RAW264.7 细胞和 Vero 细胞无细胞毒作用。LasB-IN-1 (50-100 μM, 24 h) 表现出轻微的细胞毒作用。LasB-IN-1 (0.625-10 μM, 4 h) 对小鼠和人红细胞的溶血作用可忽略不计[1]。
LasB-IN-1 (10 μM, 4, 6 h) 能有效抑制斑马鱼幼鱼巨噬细胞向损伤部位的迁移[1]。
LasB-IN-1 (0.625-10 μM, 27 h) 抑制 LPS (1 μg/mL, 24 h) 处理的 RAW264.7 细胞 中 IL-1β、TNF-α 和 IL-6 的产生。LasB-IN-1 (1.25-10 μM, 27 h) 也能抑制 COX-2、iNOS、IL-1β、TNF-α 和 IL-6 的 mRNA 表达[1]。
LasB-IN-1 (1.25-10 μM, 27 h) 显著抑制 LPS (1 μg/mL, 24 h) 处理的 RAW264.7 细胞内 NF-κB p65、i -κB α、JNK 和 ERK 的磷酸化，且呈浓度依赖性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

LasB-IN-1 相关抗体:

Cell Viability Assay[1]

Cell Line: RAW264.7 cell and Vero cell
Concentration: 1.25, 2.5, 5, 10, 20, 50, 100 μM
Incubation Time: 24 h
Result: Revealed no cytotoxic effect at concentrations of lower than 20 μM, a slight cytotoxic effect was observed at a concentration of 50 μM, indicating the noncytotoxicity at concentrations effective against virulence and biofilm formation.
体内研究
(In Vivo)

LasB-IN-1 (1, 2 mg/kg, 灌胃, 4 h) 抑制小鼠肺组织内的中性粒细胞浸润[1]。
LasB-IN-1 (1, 2 mg/kg, 灌胃, 4 h) 显著下调小鼠 IL-1β、TNF-α 和 IL-6 的表达水平，并降低 COX-2、iNOS、IL-1β、TNF-α 和 IL-6 mRNA 的表达[1]。
LasB-IN-1 (2, 4 mg/kg, 灌胃, 每日一次，7 d) 无明显不良反应[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: eight-week-old BALB/c wild-type mice (male, 18–22 g ), established a ALI model by using LPS (P. aeruginosa)[1]
Dosage: 1 and 2 mg/kg
Administration: intragastric (i.g.), after treatment for 4 h, intraperitoneal injection of LPS (20 mg/kg), sacrificed by cervical dislocation after a 6 h treatment
Result: Reduced myeloperoxidase (MPO) activity in mice compared with that in LPS-only mice, indicating the inhibition of neutrophil infiltration in mouse lung tissues.
Exhibited significantly downregulated expression levels of IL-1β, TNF-α, and IL-6, with a concentration-dependent response while significantly reduced mRNA expression of COX-2, iNOS, IL-1β, TNF-α, and IL-6 in mice compared with LPS-only mice.
Animal Model: eight-week-old BALB/c wild-type mice (male, 18–22 g )[1]
Dosage: 2 and 4 mg/kg
Administration: intragastric (i.g.) for 7 days
Result: Exhibited no adverse effects such as vomiting or diarrhea, had a negligible impact on the body weight of mice, did not induce any significant damage or histopathological alterations in vital organs.
分子量

365.39

Formula

C20H22F3NO2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

LasB-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LasB-IN-1ElastaseNF-κBp38 MAPKBacterialNuclear factor-κBNuclear factor-kappaBPseudomonas aeruginosaLasBMAPKinhibitorelastasevirulencebiofilminflammatory responsedrug-resistant infectionsRAW264.7 cellVero cellP. aeruginosa strain PAO1BALB/c wild-type miceInhibitorinhibit

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