2. Anti-infection
  3. Penicillin-binding protein (PBP) Bacterial
  4. YU253434

YU253434 是一种 PBP3 抑制剂，其与铜绿假单胞菌 PBP3 的 IC50 为 2.5 μM。YU253434 含有铁载体结构域，可促进其被革兰氏阴性杆菌的周质空间摄取。YU253434 对多重耐药革兰氏阴性杆菌具有抗菌活性。YU253434 可用于多重耐药革兰氏阴性菌感染的研究。

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YU253434

YU253434 Chemical Structure

CAS No. : 2408801-88-5

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YU253434 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YU253434 is a PBP3 inhibitor with an IC50 of 2.5 μM against Pseudomonas aeruginosa PBP3. YU253434 contains a siderophore domain that facilitates its uptake into the periplasmic space of Gram-negative bacilli. YU253434 exhibits antibacterial activity against multidrug-resistant Gram-negative bacilli. YU253434 can be used in studies of multidrug-resistant Gram-negative bacterial infections[1].

体外研究
(In Vitro)

YU253434 可强效抑制铜绿假单胞菌 (MIC50 = 1 μg/mL，MIC90 = 8 μg/mL)、肺炎克雷伯菌 (MIC50 = 1 μg/mL，MIC90 = 4 μg/mL) 和大肠埃希菌 (MIC50 = 1 μg/mL，MIC90 = 4 μg/mL) 临床分离株的生长；且随着培养基中铁水平的升高，其抗菌活性呈浓度依赖性降低[1]。
YU253434 对 A 类、C 类和 D 类丝氨酸 β-内酰胺酶的水解作用具有抗性，同时是 B 类金属 β-内酰胺酶 NDM-1、VIM-2 和 IMP-1 的弱底物[1]。

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

YU253434 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 C0 AUClast AUCinf MRT Vss CL
Mice[1] 50 mg/kg i.v. 11 h 200844 ng/mL 55866 ng·h/mL 57791 ng·h/mL 3 h 2 L/kg 14 mL/min/kg
体内研究
(In Vivo)

YU253434 (50 mg/kg；静脉注射、皮下注射；单次给药) 在 CD-1 小鼠体内展现出与静脉用 β-内酰胺类抗生素相似的快速清除特征，单次静脉注射 50 mg/kg 剂量后，其血浆浓度在至少 2 小时内维持在 1 μg/mL 的 MIC50 水平以上[1]。

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

Animal Model: CD-1 mice[1]
Dosage: 50 mg/kg (i.v.); 50 mg/kg (s.c.)
Administration: i.v.; single dose; s.c.; single dose
Result: Reached plasma concentration of 1395 ng/mL at 4 hours after intravenous administration.
Maintained plasma concentration above 1000 ng/mL at the 2-hour time point after intravenous administration.
Achieved a half-life of 11 h, initial plasma concentration (C0) of 200844 ng/mL, AUClast of 55866 h ng/mL, AUCINF of 57791 h ng/mL, mean residence time (MRT) of 3 h, volume of distribution at steady state (Vss) of 2 L/kg, and clearance (CL) of 14 mL/min/kg after intravenous administration.
Yielded nearly identical pharmacokinetic data after subcutaneous administration.
分子量

686.61

Formula

C27H26N8O12S
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

YU253434 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

YU2534342408801-88-5YU 253434YU-253434Penicillin-binding protein (PBP)Bacterialcatalytic serine residuePBP3Klebsiella pneumoniaeserine β-lactamasesmetallo-β-lactamasesEscherichia coliGram-negative bacilliβ-lactamasesPseudomonas aeruginosasiderophore moietyInhibitorinhibitorinhibit

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目录号：
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