2. Anti-infection
  3. Beta-lactamase
  4. ATM potentiator-1

ATM potentiator-1 (compound 9) 是一种 β-内酰胺酶抑制剂与外排泵抑制剂，对 NDM-1 的 IC50 为 1.6 μM，对 OXA-10 的 IC50 为 12.5 μM 和 5.4 μM，对 VIM-2 的 IC50 为 5.0 μM，对 KPC-2 的 IC50 为 26.7 μM，对 OXA-48 的 IC50 为 3.4 μM。ATM potentiator-1 可抑制 铜绿假单胞菌 的外排泵活性，与 CCCP 联用时具有叠加抑制效应。ATM potentiator-1 可用于碳青霉烯类耐药铜绿假单胞菌 (crpa) 感染的研究。

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ATM potentiator-1

ATM potentiator-1 Chemical Structure

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ATM potentiator-1 相关抗体

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Metallo-β-lactamase (MBL) Serine β-lactamase (SBL)

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ATM potentiator-1 (compound 9) is a β-lactamase inhibitor and efflux pump inhibitor, with an IC50 of 1.6 μM against NDM-1, IC50 values of 12.5 μM and 5.4 μM against OXA-10, an IC50 of 5.0 μM against VIM-2, an IC50 of 26.7 μM against KPC-2, and an IC50 of 3.4 μM against OXA-48. ATM potentiator-1 inhibits the efflux pump activity of *Pseudomonas aeruginosa* and exerts a synergistic inhibitory effect when combined with CCCP. ATM potentiators-1 can be used for the research of carbapenem-resistant *Pseudomonas aeruginosa* (CRPA) infections[1].

体外研究
(In Vitro)

ATM potentiator-1 (compound 9) (0.1, 1, 10, 70 μM; 20 min) 可抑制纯化的 β-内酰胺酶 KPC-2、NDM-1、VIM-2、OXA-48 和 OXA-10，其 IC50 值范围为 1.6 至 26.7 μM，对 NDM-1 的活性最强[1]。
ATM potentiator-1 (0, 10, 25, 50 μM; 10 min) 可结合至纯化 NDM-1 的活性位点，这一点可通过色氨酸固有荧光的浓度依赖性淬灭得到证实[1]。
ATM potentiator-1 (8 mg/L; 60 min) 可抑制产 NDM-1 的铜绿假单胞菌菌株 PA-017 中的外排泵，溴化乙锭的细胞内滞留量增加可证明这一点[1]。
ATM potentiator-1 (16 mg/L; 24 h) 可增强氨曲南对产 NDM-1 的铜绿假单胞菌菌株 PA-017 的活性，将氨曲南的 MIC 从 16 mg/L 降至 1 mg/L[1]。
ATM potentiator-1 (1, 2, 4, 8, 16, 32 mg/L; 18-24 h) 可增强氨曲南对 29 株产碳青霉烯酶的耐碳青霉烯铜绿假单胞菌分离株的活性，其中 93%的菌株显示出协同作用 (FICI ≤0.5)，且氨曲南的 MIC 降低≥4 倍[1]。
ATM potentiator-1 (1, 2, 4, 8, 16, 32 mg/L) 不会使产 NDM-1 的铜绿假单胞菌菌株 PA-017 的外膜通透，NPN 荧光无变化的结果可证明这一点[1]。
ATM potentiator-1 (0.5, 1, 2, 4, 8, 16, 32 mg/L; 24 h) 不会降低永生化人胚肾 HEK293 细胞孵育 24 h 后的存活率[1]。
ATM potentiator-1 (4, 8, 16, 32 mg/L; 30 min) 在 37 °C 孵育 30 min 后不会导致人红细胞溶血[1]。

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

ATM potentiator-1 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: Immortalized human embryonic kidney (HEK293) cells
Concentration: 0.5, 1, 2, 4, 8, 16, 32 mg/L
Incubation Time: 24 h
Result: Did not affect HEK293 cell viability at concentrations up to 32 mg/L.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Cmax AUC0-last AUC0-∞ MRT0-last MRT0-∞ C0 Vss Vz CL
Rat[1] 5 mg/kg i.v. 1.44 h 6.96 mg/L 2.55 mg·h/L 2.61 mg·h/L 0.63 h 0.85 h 13.23 mg/L 3.45 L/kg 1.00 L/kg 2000 mL/h/kg
体内研究
(In Vivo)

ATM potentiator-1 (compound 9) (腹腔注射，每次 40 mg/kg，共给药 4 次，间隔 2 小时，联合 20 mg/kg 氨曲南) 可在产 NDM-1 的铜绿假单胞菌小鼠大腿感染模型中使细菌载量降低 3.4 log10[1]。
ATM potentiator-1 (10-40 mg/kg；腹腔注射；单次给药) 在 6 周龄雌性 C57BL/6J 小鼠中耐受性良好，7 天内存活率为 100%[1]。

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

Animal Model: C57BL/6J mice (7 week-old female, 20-22 g, intramuscular thigh infection with NDM-1-producing Pseudomonas aeruginosa strain PA-017)[1]
Dosage: 40 mg/kg (in combination with 20 mg/kg aztreonam)
Administration: i.p.; 4 total doses at 2-hour intervals
Result: Reduced mean bacterial burden in thigh tissue to 4.26 log10 CFU/thigh, representing a 3.4 log10 drop compared to untreated control.
Achieved a greater reduction than aztreonam alone (2.2 log10 drop).
Reduced thigh muscle weight by 26.4% compared to untreated control.
Caused no significant body weight changes or overt clinical signs.
Animal Model: C57BL/6J mice (6 week-old female)[1]
Dosage: 10 mg/kg; 20 mg/kg; 40 mg/kg
Administration: i.p.; single dose
Result: Resulted in 100% survival of mice over the 7-day observation period for all doses.
分子量

472.44

Formula

C23H22F2N4O5
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

ATM potentiator-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:

ATM potentiator-1ATM potentiator1ATM potentiator 1Beta-lactamaseβ-lactamaseHEK293 cellsPseudomonas aeruginosaβ-lactamase inhibitorKPC-2OXA-10OXA-48murine thigh infection modelNDM-1efflux pump inhibitorVIM-2Inhibitorinhibitorinhibit

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