1. Anti-infection
  2. Bacterial
  3. MK-7762

MK-7762 是一种具有口服抗结核活性的噁唑烷酮类化合物。MK-7762 可抑制 MAO-B 及哺乳动物线粒体蛋白质合成。MK-7762 可降低急性和慢性结核感染 BALB/c 小鼠模型的肺部细菌载量,穿透 C3HeB/FeJ 小鼠的干酪样坏死肺部病灶,并在病灶区维持高于游离 MIC 的浓度。MK-7762 可用于结核病的相关研究。

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MK-7762

MK-7762 Chemical Structure

CAS No. : 2706576-88-5

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MK-7762 is an orally active xazolidinone compound with antitubercular activity. MK-7762 inhibits MAO-B and mammalian mitochondrial protein synthesis. MK-7762 reduces lung bacterial burden in BALB/c mouse models of acute and chronic tuberculosis infection, penetrates caseous necrotic lung lesions in C3HeB/FeJ mice, and maintains concentrations above unbound MIC in lesion compartments. MK-7762 can be used for the research of tuberculosis[1].

体外研究
(In Vitro)

MK-7762 (0.93 μM; 7 天) 可抑制 95% 的Mycobacterium tuberculosis (Mtb) 生长[1]
MK-7762 (72 h) 可抑制 HepG2 细胞中的哺乳动物线粒体蛋白质合成,其 IC50 为 98 μM[1]
MK-7762 (18.1 μM;7 天) 可杀灭 99% 的 H37Rv 细胞[1]
MK-7762 (10 μM) 可抑制 MAO-B,其 IC50 为 6.9 μM[1]

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

体内研究
(In Vivo)

MK-7762 (30-100 mg/kg;灌胃;每日 1 或 2 次;连续 12 天) 可降低急性感染的BALB/c小鼠肺部细菌载量[1]
MK-7762 (30-200 mg/kg;灌胃;每日 1 次;持续 1 个月) 可降低慢性感染 BALB/c 小鼠的肺部细菌载量[1]
MK-7762 (100 mg/kg;灌胃;每日 1 次,每周 5 天;持续 2.5 周) 可穿透 C3HeB/FeJ 小鼠的干酪样坏死病灶,且病灶内药物浓度高于游离 MIC[1]

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

Animal Model: BALB/c (female, 6-8 weeks old, specific-pathogen-free, acute Mtb infection)[1]
Dosage: 30 mg/kg; 100 mg/kg
Administration: I.g.; once daily, twice daily; 12 days
Result: Achieved 1.4-log reduction in lung CFUs (30 mg/kg once daily).
Achieved 4.5-log reduction in lung CFUs (100 mg/kg once daily).
Achieved 5.3-log reduction in lung CFUs (100 mg/kg twice daily) versus untreated controls.
Animal Model: BALB/c (female, 6-8 weeks old, specific-pathogen-free, chronic Mtb infection)[1]
Dosage: 30 mg/kg; 100 mg/kg; 200 mg/kg
Administration: I.g.; once daily; 1 month
Result: Achieved 0.7-log reduction in lung CFUs (30 mg/kg).
Achieved 1.9-log reduction in lung CFUs (100 mg/kg).
Achieved 2.2-log reduction in lung CFUs (200 mg/kg) versus untreated controls.
分子量

419.40

Formula

C16H19F2N3O6S

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
  • 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.

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MK-7762
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HY-181146
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