1. Anti-infection
  2. Influenza Virus
  3. Influenza A virus-IN-19

Influenza A virus-IN-19 (Compound (S)-63) 是一种具有口服活性、选择性的 Influenza A virus 抑制剂,EC50 为 0.44 μM。Influenza A virus-IN-19 对 Hemagglutinin 表现出中等的结合亲和力,Kd 为 5.66 μM。Influenza A virus-IN-19 抑制胰蛋白酶介导的 HA0 切割,阻断病毒早期侵入过程,并抑制甲型流感病毒的复制。Influenza A virus-IN-19 可提高致死性流感小鼠模型的存活率。Influenza A virus-IN-19 可用于甲型流感病毒感染的相关研究。

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Influenza A virus-IN-19

Influenza A virus-IN-19 Chemical Structure

CAS No. : 3027187-19-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Influenza A virus-IN-19 (Compound (S)-63) is an orally active, selective Influenza A virus inhibitor with an EC50 of 0.44 μM. Influenza A virus-IN-19 exhibits moderate binding affinity to Hemagglutinin, with a Kd of 5.66 μM. Influenza A virus-IN-19 inhibits trypsin-mediated cleavage of HA0, blocks the early viral entry process, and suppresses the replication of Influenza A virus. Influenza A virus-IN-19 improves the survival rate of mice in lethal influenza models. Influenza A virus-IN-19 can be used in studies related to Influenza A virus infection[1].

体外研究
(In Vitro)

Influenza A virus-IN-19 可强效抑制 MDCK 细胞中的甲型流感病毒 H1N1 (A/FM/1/47),其 EC50 为 0.44 μM,选择指数为 210.75[1]
Influenza A virus-IN-19 可强效抑制 MDCK 细胞中耐 Oseltamivir (HY-13317) 的甲型流感病毒 H1N1 (A/Tianjin Jinnan/15/2009),其 EC50 为 0.23 μM,选择性指数为 403.17;同时可抑制甲型流感病毒 H3N2 (A/HanFang/359/95),EC50 为 12.11 μM,选择性指数为 5.51[1]

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

药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Cmax AUC0-inf MRT0-inf Tmax F
Mice[1] 2 mg/kg i.v. 1.32 h 1257 ng/mL 520 ng·h/mL 0.76 h / /
Mice[1] 50 mg/kg p.o. 4.30 h 1389 ng/mL 5041 ng·h/mL 5.02 h 0.67 h 38.78 %
体内研究
(In Vivo)

Influenza A virus-IN-19 (口服,感染前给 1 次,随后每日给 2 次,持续 7 天,剂量 5-45 mg/kg) 对致死性流感感染的雌性 KM 小鼠具有保护作用[1]

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

Animal Model: KM mice (female, 13−15 g, intranasally infected with 3 LD50 of mouse-adapted influenza virus A/Puerto Rico/8/1934)[1]
Dosage: 5 mg/kg; 15 mg/kg; 45 mg/kg
Administration: p.o.; once pre-infection, then twice daily; 7 days
Result: Provided 0% survival at 5 mg/kg.
Achieved 20% survival at 15 mg/kg.
Resulted in 0% survival due to treatment-related toxicity at 45 mg/kg.
Caused progressive body weight loss across all treatment groups; surviving mice began to regain weight following treatment discontinuation.
分子量

390.26

Formula

C16H14Cl2FNO3S

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.

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参考文献
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Influenza A virus-IN-19
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HY-182895
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