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编 号：F756848
分子式：C27H26ClNO7
分子量：511.95
分子式：C27H26ClNO7
分子量：511.95
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CAS No: 2919303-26-5
产品详情
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.
体内研究：
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。Pharmacokinetic (PK) Profile In Vivo of Influenza virus-IN-6 (Compound 35) after a Single Dose in Rats In Vivo (n = 5)aparameterIV (2 mg/kg) PO (10 mg/kg) IP (15 mg/kg)
T1/2 (h)0.33 ± 0.070.82 ± 0.161.07 ± 0.25
Tmax (h)NA0.520.45
Cmax (ng/mL)1586.55 ± 366.4892.20 ± 36.25889.52 ± 233.17
AUC0-t (h·ng/mL)536.45 ± 58.72164.30 ± 26.37790.62 ± 188.31
CL (mL/min/kg)53.76 ± 13.18NANA
F %NA6.13%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.Animal Model:Balb/C mice, H1N1 infection model
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
Dosage:2, 10 or 15 mg/kg
Administration:IV, IP, or PO (Pharmacokinetic Analysis)
Result:Showed good pharmacokinetic profiles.
体外研究：
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。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。Influenza virus-IN-6 (2.5-10 μM; 24 h) 抑制流感病毒聚合酶活性。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。
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.
体内研究：
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。Pharmacokinetic (PK) Profile In Vivo of Influenza virus-IN-6 (Compound 35) after a Single Dose in Rats In Vivo (n = 5)aparameterIV (2 mg/kg) PO (10 mg/kg) IP (15 mg/kg)
T1/2 (h)0.33 ± 0.070.82 ± 0.161.07 ± 0.25
Tmax (h)NA0.520.45
Cmax (ng/mL)1586.55 ± 366.4892.20 ± 36.25889.52 ± 233.17
AUC0-t (h·ng/mL)536.45 ± 58.72164.30 ± 26.37790.62 ± 188.31
CL (mL/min/kg)53.76 ± 13.18NANA
F %NA6.13%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.Animal Model:Balb/C mice, H1N1 infection model
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
Dosage:2, 10 or 15 mg/kg
Administration:IV, IP, or PO (Pharmacokinetic Analysis)
Result:Showed good pharmacokinetic profiles.
体外研究：
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。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。Influenza virus-IN-6 (2.5-10 μM; 24 h) 抑制流感病毒聚合酶活性。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。
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