2. Anti-infection
  3. Bacterial
  4. Antitubercular agent-56

Antitubercular agent-56 是 Questiomycin A (HY-N8439) 的衍生物，是一种高效且口服有效的抗结核剂。Antitubercular agent-56 通过抑制 FabD (Kd = 9.39 μM；IC50 = 49.60 μM) 破坏结核分枝杆菌的细胞膜完整性。Antitubercular agent-56 在体外和体内均表现出对 Mycobacterium tuberculosis (MTB) 及耐药 MTB 良好的细胞内抗分枝杆菌活性。Antitubercular agent-56 可用于结核病 (TB) 的相关研究。

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Antitubercular agent-56

Antitubercular agent-56 Chemical Structure

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Customer Review

Antitubercular agent-56 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

Antitubercular agent-56, a Questiomycin A (HY-N8439) derivative, is a potent and orally active antitubercular agent. Antitubercular agent-56 disrupts mycobacterial envelope integrity by inhibiting FabD (Kd = 9.39 μM; IC50 = 49.60 μM). Antitubercular agent-56 exhibits good intracellular antimycobacterial activity against Mycobacterium tuberculosis (MTB) and drug-resistant MTB both in vitro and in vivo. Antitubercular agent-56 can be used for research on tuberculosis (TB)[1].

IC50 & Target

FabD

9.39 μM (Kd)

FabD

49.60 μM (IC50)

体外研究
(In Vitro)

Antitubercular agent-56 (compound B10) (7 天) 对结核分枝杆菌 H37Rv (MIC = 0.15 μg/mL) 以及对药敏和耐药的结核分枝杆菌菌株均表现出强效的抗结核活性，其 MIC 范围为 0.063 至 0.25 μg/mL[1]。
Antitubercular agent-56 (0.26-64 μg/mL，48 小时) 对 Vero、HepG2 和 J774A.1 细胞表现出低细胞毒性，其 IC50 分别为 > 128、> 80 和 > 80 μg/mL[1]。
Antitubercular agent-56 (1/2 × MIC-16 × MIC；0-14 天) 在浓度和时间依赖性方式下对 H37Rv 结核分枝杆菌菌株及临床分离株表现出强效的杀菌活性[1]。

Antitubercular agent-56 (1-4 μg/mL；72 小时) 能有效穿透巨噬细胞，并抑制胞内结核分枝杆菌 (MTB) 的生长[1]。
Antitubercular agent-56 (4 × MIC；30 分钟) 显著增加了分枝杆菌膜的通透性，证实了其对细胞壁完整性的破坏作用[1]。

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

Antitubercular agent-56 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Mice[1] 10 nM p.o. T1/2 5.34 h
Mice[1] 10 nM p.o. Tmax 0.5 h
Mice[1] 10 nM p.o. Cmax 229.97 ng/mL
Mice[1] 10 nM p.o. AUC0-24 738.12 ng·h/mL
体内研究
(In Vivo)

Antitubercular agent-56 (compound B10) (100 mg/kg；灌胃；每周 5 次，持续 3 周) 可降低感染结核分枝杆菌的小鼠肺部细菌负荷[1]。
Antitubercular agent-56 (500 mg/kg；灌胃；单次给药) 在小鼠中表现出良好的安全性特征[1]。

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

Animal Model: Female BALB/c mice (18-20 g) infected with Mycobacterium tuberculosis H37Ra strain[1]
Dosage: 100 mg/kg
Administration: i.g.; five times weekly for 3 weeks
Result: Induced little reductions in mean lung bacterial burden, demonstrating log10 CFU decreases of 0.84.
Showed inhibitory activity against Mycobacterium tuberculosis H37Ra.
Animal Model: Female BALB/c mice (17-20 g)[1]
Dosage: 500 mg/kg
Administration: i.g.; single dose
Result: Showed all mice survived without any abnormalities compared to control.
Showed no significant changes in body weight.
分子量

295.29

Formula

C16H13N3O3
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

Antitubercular agent-56 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:

Antitubercular agent-56Antitubercular agent56Antitubercular agent 56Bacterialmycobacterial envelope integrityintracellular antimycobacterial activityMDR-TBtuberculosisMycobacterium tuberculosismycolic acid biosynthesismacrophagesFabDInhibitorinhibitorinhibit

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目录号：
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