2. Anti-infection
  3. Antibiotic
  4. BB-3497

BB-3497 是一种强效、具有口服活性且选择性强的肽去甲酰酶 (PDF) 抑制剂。BB-3497 对 PDF 具有高度选择性 (对大肠杆菌 PDF.Ni 的 IC50 = 7 nM)，对其他哺乳动物金属酶 (MMP-1/2/3/7 和脑啡肽酶) 的选择性较低。BB-3497 对革兰氏阳性菌和某些革兰氏阴性病原体均表现出强效抗菌活性。在系统性金黄色葡萄球菌感染小鼠模型中，BB-3497 可保护小鼠免受感染。BB-3497 可用于抗细菌感染相关研究。

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BB-3497

BB-3497 Chemical Structure

CAS No. : 235784-88-0

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BB-3497 相关抗体

Top Publications Citing Use of Products

查看 Antibiotic 亚型特异性产品:

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Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BB-3497 is a potent, orally active and selective peptide deformylase (PDF) inhibitor. BB-3497 is highly selective for PDF (IC50 = 7 nM for E. coli PDF.Ni) over the other mammalian metalloenzymes (MMP-1/2/3/7 and enkephalinase). BB-3497 exhibits potent activity against gram-positive bacteria and some gram-negative pathogens. BB-3497 protects mice from infection in systemic models of Staphylococeus aureus. BB-3497 can be used for anti-bacterial infection research[1].

体外研究
(In Vitro)

BB-3497 与 PDF 结合，其 N- 甲酰羟胺基团的氧原子占据了 PDF-Met-Ala-Ser 产物复合物中观察到的两个镍结合水分子的位置[1]。
BB-3497 对携带对照质粒 (pET24) 或 pET24-PDF 的大肠杆菌 DH5α 和 BL21 (DE3) 菌株表现出优异的体外抗菌活性，MIC 值分别为 4、8、32 和 128 μg/mL，但对大肠杆菌甲酰转移酶突变株的 MIC 值 >128 μg/mL，证实其抗菌作用是通过抑制 PDF 实现的[1]。
BB-3497 (4-8 倍 MIC，24 小时) 可使金黄色葡萄球菌和大肠杆菌的活菌数下降不到 1 个对数单位，证实了其抑菌作用[1]。
BB-3497 (2-4 倍 MIC，24 小时) 可使大肠杆菌和金黄色葡萄球菌分别产生 1×10-7 倍和 2×10-7 倍的耐药突变株，其中高水平耐药由 fmt 基因突变所导致，而低水平耐药突变株则具有野生型的 def-fmt 操纵子[1]。

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

BB-3497 相关抗体:
体内研究
(In Vivo)

BB-3497 (3-100 mg/kg，口服或静脉注射，感染后 1 小时单次给药) 可保护小鼠免受金黄色葡萄球菌和耐甲氧西林金黄色葡萄球菌的感染[1]。

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

Animal Model: Male ICR-derived mice intraperitoneally inoculated with S. aureus[1]
Dosage: 3, 6, 10, 30, 60 and 100 mg/kg
Administration: p.o. or i.v., single dose at 1 h after bacterial challenge
Result: Rescued mice from infection with an ED50 of 7 mg/kg (i.v.) and 8 mg/kg (p.o.), respectively.
Animal Model: Male ICR-derived mice intraperitoneally inoculated with methicillin-resistant S. aureus[1]
Dosage: 3, 6, 10, 30, 60 and 100 mg/kg
Administration: p.o., single dose at 1 h after bacterial challenge
Result: Showed an ED50 of 14 mg/kg.
分子量

329.44

Formula

C16H31N3O4
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

BB-3497 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:

BB-3497235784-88-0BB3497BB 3497AntibioticPDFStaphylococeus aureusE. coliformyltransferase mutantantibacterialICR-derived miceInhibitorinhibitorinhibit

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