1. Metabolic Enzyme/Protease Anti-infection
  2. Elastase Bacterial
  3. LasB-IN-3

LasB-IN-3 是铜绿假单胞菌 (Pseudomonas aeruginosa) 的弹性蛋白酶 (LasB) 抑制剂,其 IC50 值为 8.5 nM。LasB-IN-3 对 Met128Val 突变体的 IC50 为 58.9 nM。LasB-IN-3 可结合野生型及 Met128Val 突变体 LasB 的活性位点,螯合锌离子,形成氢键与 CH-π 相互作用,从而抑制 LasB 的蛋白水解活性。LasB-IN-3 可提高 LasB 诱导的急性肺损伤小鼠模型的存活率。LasB-IN-3 可用于铜绿假单胞菌 (Pseudomonas aeruginosa) 感染的相关研究。

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LasB-IN-3

LasB-IN-3 Chemical Structure

CAS No. : 2762675-42-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LasB-IN-3 is a protease elastase (LasB) inhibitor of Pseudomonas aeruginosa with an IC50 value of 8.5 nM. LasB-IN-3 shows an IC50 of 58.9 nM for the Met128Val mutant. LasB-IN-3 binds to active sites of wild-type and Met128Val mutant LasB, coordinates zinc ions, forms hydrogen bonds and CH-π interactions, and inhibits LasB proteolytic activity. LasB-IN-3 increases survival rate in LasB-induced acute lung injury mice models. LasB-IN-3 can be used for the research of Pseudomonas aeruginosa infection[1].

体外研究
(In Vitro)

LasB-IN-3 (Compound 21) 可强效抑制野生型铜绿假单胞菌 LasB,其 IC50 为 8.5 ± 0.5 nM;其对 Met128Val 突变体的活性降低了约 7 倍 (IC50 = 58.9 nM)[1]
LasB-IN-3 可在猪肺表面活性物质存在的情况下抑制铜绿假单胞菌 LasB,其 IC50 为 45 nM,活性降低的原因是其与表面活性蛋白的结合率达 37.2 ± 0.8%[1]
LasB-IN-3 (0-100 μM) 对人源 A549、HepG2 和 HEK293 细胞系仅表现出极低的细胞毒性[1]

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

药代动力学
(Parmacokinetics)
Species Dose Route T1/2 C0 AUC0-t MRT Vz CL_obs
Mice[1] 2 mg/kg i.v. 2.30 ± 0.4 h 8.55 ± 6.96 μg/mL 4.68 ± 1.18 μg/mL·h 2.8 ± 0.6 h 1.19 ± 0.4 L/kg 5.89 ± 1.2 mL/min/kg
体内研究
(In Vivo)

LasB-IN-3 (Compound 21) (300 μM;鼻内滴注) 可使经 LasB 诱导的急性肺损伤攻毒的 C57BL/6 小鼠的存活率达到 100%[1]

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

Animal Model: C57BL/6 (8-week-old male; acute lung injury model via intranasal instillation of 40 μg purified Pseudomonas aeruginosa LasB elastase)[1]
Dosage: 300 μM
Administration: intranasal; single dose (preincubated with LasB prior to instillation)
Result: Achieved 100% survival over 7 days.
分子量

381.79

Formula

C18H21ClNO4P

CAS 号
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
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  • 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.

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产品名称:
LasB-IN-3
目录号:
HY-181647
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