1. Anti-infection
  2. Bacterial
  3. JNJ-6640

JNJ-6640 是一种靶向分枝杆菌 PurF (从头合成嘌呤生物合成途径中的第一个酶) 的抑制剂,具有强大的抗结核活性。JNJ-6640 在体外对结核分枝杆菌具有杀菌活性,其 MIC90 为 8.6 nM。JNJ-6640 干扰从头嘌呤生物合成,抑制体内 Mycobacterium tuberculosis 的 DNA 复制。JNJ-6640 在急性感染小鼠中展现出抗结核疗效。JNJ-6640 可用于结核病研究。

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JNJ-6640

JNJ-6640 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JNJ-6640 is an inhibitor targeting mycobacterial PurF (the first enzyme in the de novo purine biosynthesis pathway) with potent anti-tuberculosis activity. JNJ-6640 exhibits bactericidal activity against Mycobacterium tuberculosis in vitro, with an MIC90 of 8.6 nM. JNJ-6640 disrupts de novo purine biosynthesis, inhibits M. tuberculosis DNA replication in vivo. JNJ-6640 exhibits anti-tuberculosis efficacy in acutely infected mice. JNJ-6640 can be used for the study of tuberculosis[1].

体外研究
(In Vitro)

JNJ-6640 对 Mycobacterium tuberculosis H37Rv 菌株表现出强大的体外抑制和杀菌活性,最小抑菌浓度 (MIC90) 为 8.6 nM,最小杀菌浓度 (MBC99.9) 为 140 nM;在胆固醇培养基中,(MIC90) 为 29.1 nM;对于 THP-1 巨噬细胞内的 M. tuberculosis,IC50 为 26.1 nM[1]
JNJ-6640 (100 nM, 4 h) 显著降低 M. tuberculosis15N 掺入腺嘌呤和腺苷单磷酸 (AMP) 的比例[1]
JNJ-6640 (1 nM) 抑制 M. tuberculosis PurF 酶[1]
JNJ-6640 (0.6 μM, 6-10 h) 阻滞表达 TdTomato 的 M. tuberculosis 的生长[1]

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

体内研究
(In Vivo)

JNJ-6640 (1500 mg/kg,皮下注射长效制剂,每周一次,持续 2-8 周) 在急性感染的雌性 Balb/cBy 小鼠中表现出抗结核疗效[1]

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

Animal Model: Mycobacterium tuberculosis H37Rv (200 CFU) was intranasally inoculated into 6-8-week-old female Balb/cBy mice to construct an acute tuberculosis infection model[1]
Dosage: 1500 mg/kg
Administration: s.c. injection of LAI, once weekly for 2, 8 weeks
Result: Reduced lung bacterial load.
Showed no significant changes in body weight and no obvious clinical signs of toxicity.
Reduced the phosphorylation of molecules related to M. tuberculosis DNA replication in mice.
分子量

340.35

Formula

C17H17FN6O

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

JNJ-6640 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 *
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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.

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JNJ-6640
目录号:
HY-177105
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