1. Anti-infection
  2. Influenza Virus
  3. Influenza virus-IN-6

Influenza virus-IN-6 (Compound 35) 是一种有效的流感聚合酶酸性蛋白亚基内切酶 N 端结构域 (PAN) 抑制剂,IC50 为 0.20 μM。

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Influenza virus-IN-6 Chemical Structure

Influenza virus-IN-6 Chemical Structure

CAS No. : 2919303-26-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Influenza virus-IN-6 (Compound 35) is a potent influenza N-terminal domain of the polymerase acidic protein subunit (PAN) endonuclease inhibitor with an IC50 of 0.20 μM[1].

IC50 & Target

IC50: 0.20 μM (PAN)[1]
KD: 56.02 nM (PAN)[1]

体外研究
(In Vitro)

Influenza virus-IN-6 (Compound 35) (48 h) 具有有抗流感病毒活性,在 MDCK 细胞中对 H1N1、H5N1、H3N2 和 Flu B 的 EC50 分别为 1.28 ± 0.35、1.12 ± 0.65、0.76 ± 0.11 和 0.43 ± 0.06 μM[1]
Influenza virus-IN-6 (5-20 μM; 24 h) 影响病毒复制,但不影响病毒颗粒、细胞和吸附[1]
Influenza virus-IN-6 (2.5-10 μM; 24 h) 抑制流感病毒聚合酶活性[1]
Influenza virus-IN-6 在小鼠血浆、肝微粒体和肠道 S9-UDPGA 中显示出良好的稳定性[1]

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

Western Blot Analysis[1]

Cell Line: MDCK cells
Concentration: 5, 10 and 20 μM
Incubation Time: 24 h
Result: Decreased nucleoprotein (NP) and matrix protein 2 (M2).

RT-PCR[1]

Cell Line: MDCK cells
Concentration: 2.5, 5, 10 and 20 μM
Incubation Time: 24 h
Result: Decreased the expression of viral NP mRNA in a well-defined dose-dependent manner. Inhibited cRNA synthesis in a dose-dependent fashion.
体内研究
(In Vivo)

Influenza virus-IN-6 (Compound 35) (7.5-30 mg/kg/d; i.p.; twice daily for 7 days) 显著保护小鼠免受流感病毒感染[1]
Pharmacokinetic (PK) Profile In Vivo of Influenza virus-IN-6 (Compound 35) after a Single Dose in Rats In Vivo (n = 5)a[1]

parameter IV (2 mg/kg) PO (10 mg/kg) IP (15 mg/kg)
T1/2 (h) 0.33 ± 0.07 0.82 ± 0.16 1.07 ± 0.25
Tmax (h) NA 0.52 0.45
Cmax (ng/mL) 1586.55 ± 366.48 92.20 ± 36.25 889.52 ± 233.17
AUC0-t (h·ng/mL) 536.45 ± 58.72 164.30 ± 26.37 790.62 ± 188.31
CL (mL/min/kg) 53.76 ± 13.18 NA NA
F % NA 6.13% 29.50%

aIV represents intravenous injection, IP represents intraperitoneal injection, and PO represents the gastrointestinal route. T1/2 is the half-life of the compound exposure in plasma. Tmax is the time taken to reach the maximum concentration. Cmax represents the highest observed concentration. AUC (0–t) is the area under the curve. CL (mL/min/kg) is the clearance. F % is the percent bioavailability.

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

Animal Model: Balb/C mice, H1N1 infection model[1]
Dosage: 0, 7.5, 15, and 30 mg/kg/d
Administration: Intraperitoneal injection, twice per day for 7 days
Result: Exhibited excellent anti-IAV activity in vivo at a dose of 30 mg/kg/d. Still showed potent antiviral activity in vivo, with a survival ratio of approximately 60% against lethal virus infection in mice at 15 mg/kg/d.
Animal Model: SD rats[1]
Dosage: 2, 10 or 15 mg/kg
Administration: IV, IP, or PO (Pharmacokinetic Analysis)
Result: Showed good pharmacokinetic profiles.
分子量

511.95

Formula

C27H26ClNO7

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

Influenza virus-IN-6 相关分类

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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.

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