1. Anti-infection
  2. Antibiotic Bacterial
  3. Grepafloxacin

Grepafloxacin  (Synonyms: OPC-17116; dl-Grepafloxacin)

目录号: HY-A0147
产品使用指南 技术支持

Grepafloxacin (OPC-17116) 是一种口服活性氟喹诺酮类抗生素 (antibiotic),对包括肺炎链球菌在内的社区获得性呼吸道病原体具有有效活性。Grepafloxacin 具有较高的组织渗透性和良好的药效学特性。

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Grepafloxacin Chemical Structure

Grepafloxacin Chemical Structure

CAS No. : 119914-60-2

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Grepafloxacin 的其他形式现货产品:

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Other Forms of Grepafloxacin:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Grepafloxacin (OPC-17116) is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin has high tissue penetration and a promising pharmacodynamic profile[1][2][3].

IC50 & Target

Quinolone

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
> 50 μM
Compound: 45, Grepa-floxacin
Inhibition of human ERG potassium channel in HEK293 cells by patch clamp assay
Inhibition of human ERG potassium channel in HEK293 cells by patch clamp assay
[PMID: 16931010]
体外研究
(In Vitro)

格雷帕沙星 (OPC-17116;0-1 mg/L;14-21 天) 具有抗生素活性,对大肠杆菌的 MIC 值≤ 0.006 mg/L。coli strain[1]
Grepafloxacin (0-1 mg/L;3 h) 对巨噬细胞中的分枝杆菌具有抗菌活性,MIC 值为 0.5 mg/L M。avium[1]
Grepafloxacin 对肺炎链球菌等革兰氏阳性菌具有强效的体外抗菌活性,对革兰氏菌引起的实验性全身感染具有较高的体内疗效-阳性和阴性细菌检测[4]

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

体内研究
(In Vivo)

Grepafloxacin (OPC-17116;200 mg/kg;口服;Balb/c 小鼠) 在光毒性方面表现出良好的安全性[2]
Grepafloxacin (25-200 mg/kg;Balb/c 小鼠) 口服每周 5 天,持续 4 周;雌性 C57BL6/J-Lyst bg-J/ 小鼠/米色小鼠) 在鼻内 (IN) 感染和静脉内 (IV) Mycobacterium avium 感染中具有适度活动模型[3]

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

Animal Model: Female Balb/c mice (5-6 weeks)[2]
Dosage: 200 mg/kg
Administration: Oral administration; once
Result: Had mild and short-lived erythema and no changed auricular thickness.
Animal Model: Female C57BL6/J-Lyst bg-J/ mice/beige mice with mycobacterium avium infection[3]
Dosage: 25, 50, 100, and 200 mg/kg
Administration: Oral administration; 5 days/week for 4 weeks
Result: Had bactericidal activity and limited the growth of the bacteria.
分子量

359.39

Formula

C19H22FN3O3

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

Grepafloxacin 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.

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