2. Anti-infection
  3. RSV
  4. CGR-51

CGR-51 是一种口服有效的呼吸道合胞病毒 (RSV) 融合糖蛋白 (F protein) 抑制剂 (在 HEp-2 细胞中，对 RSV A2 毒株的 EC50 = 19.4 nM)。CGR-51 通过与 F 蛋白结合 (KD = 0.1 μM) 并抑制膜融合来阻断 RSV 入侵，这一机制不同于法尼基转移酶抑制。CGR-51 在体外传代过程中筛选出 RSV F 蛋白中的 K399N 抗性突变。CGR-51 可在 RSV 感染的 BALB/c 小鼠模型中有效抑制病毒复制。CGR-51 可用于 RSV 感染的相关研究。

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CGR-51

CGR-51 Chemical Structure

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CGR-51 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

CGR-51 is an orally active potent RSV fusion glycoprotein (F protein) inhibitor (EC50 = 19.4 nM against RSV A2 in HEp-2 cells). CGR-51 blocks RSV entry by binding to the F protein (KD = 0.1 μM) and inhibiting membrane fusion, a mechanism distinct from farnesyltransferase inhibition. CGR-51 selects for the K399N resistance mutation in the RSV F protein during in vitro passage. CGR-51 effectively suppresses RSV replication in a BALB/c mouse model of RSV infection. CGR-51 can be used for RSV infection research[1].

体外研究
(In Vitro)

CGR-51 (72 小时) 在 HEp-2 细胞中表现出对一组呼吸道合胞病毒 (RSV) 菌株的强效广谱活性 (对 A1540 的 EC50 = 18.2 nM，对 B9320 的 EC50 = 46.5 nM，对 B1 的 EC50 = 39.7 nM)[1]。
CGR-51 (72 小时) 在 HEp-2 细胞中的 CC50 值为 19.4 μM，并具有更高的选择性指数 (SI = 1070.9) ，表明其相较于 Lonafarnib (HY-15136) 有更优良的安全性[1]。
CGR-51 (5 μM，2-26 小时) 主要通过抑制 RSV F 蛋白介导的病毒融合，进而阻断病毒进入宿主细胞来发挥其抗病毒效应[1]。
CGR-51 (1-10 μM，24 小时) 以剂量依赖的方式通过直接靶向病毒 F 蛋白来抑制 RSV 感染，该作用不依赖于法尼基转移酶的抑制，且不诱导磷脂沉积[1]。
CGR-51 对 K399N 突变病毒的活性显著降低，EC50 和 EC90 分别比野生型病毒提高了 10.09 倍和 6.87 倍[1]。

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

CGR-51 相关抗体:
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value Note
Mice 100 mg/kg i.g. Cmax 35167 μg/L CD-1 Mice
Rat 10 mg/kg i.g. Cmax 700.56 μg/L
Rat 2 mg/kg i.v. AUC0-∞ 1103.23 μg/L·h
Mice 100 mg/kg i.g. Tmax 2.00 h CD-1 Mice
Rat 10 mg/kg i.g. AUC0-∞ 4018.85 μg/L·h
Rat 2 mg/kg i.v. T1/2 1.63 h
Mice 100 mg/kg i.g. AUC0-∞ 367319 μg/L·h CD-1 Mice
Rat 10 mg/kg i.g. T1/2 2.00 h
Mice 100 mg/kg i.g. T1/2 2.56 h CD-1 Mice
Rat 10 mg/kg i.g. Vd/F 7.37 L/kg
Rat 10 mg/kg i.g. CL 2.61 L/h/kg
Rat 10 mg/kg i.g. F 72.86 %
体内研究
(In Vivo)

CGR-51 (20 和 40 mg/kg，口服，每日两次，持续 4 天) 剂量依赖性地减轻了 BALB/c 小鼠中 RSV 诱发的肺损伤[1]。

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

Animal Model: Female BALB/c mice (10 weeks old) intranasally inoculated with RSV A2[1]
Dosage: 20 and 40 mg/kg
Administration: p.o., BID for 4 days
Result: Exhibited antiviral efficacy comparable to the 40 mg/kg dose of Lonafarnib at 20 mg/kg.
Led to a substantial reduction in both pulmonary viral titers and RNA levels at 40 mg/kg.
Demonstrated effects similar to those observed in Lonafarnib (40 mg/kg) group, showing notable improvement in lung injury at 20 mg/kg.
Provided even greater alleviation of lung damage at 40 mg/kg.
分子量

656.81

Formula

C27H30Br2ClFN4O2
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

CGR-51 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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:

CGR-51CGR51CGR 51RSVRespiratory syncytial virusF proteinfarnesyltransferaseK399NHEp-2 CellsphospholipidosisRSV A2BALB/cInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-178151
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