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2919303-26-5

2919303-26-5 Structure

2919303-26-5 Structure
IdentificationBack Directory
[Name]

Influenza virus-IN-6
[CAS]

2919303-26-5
[Synonyms]

Influenza virus-IN-6
Hazard InformationBack Directory
[Uses]

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].
[in vivo]

Influenza virus-IN-6 (Compound 35) (7.5-30 mg/kg/d; i.p.; twice daily for 7 days) markedly protects mice from influenza virus infection[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]

parameterIV (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[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.
[References]

[1] Liao Y, et al. Identification of N- and C-3-Modified Laudanosoline Derivatives as Novel Influenza PAN Endonuclease Inhibitors. J Med Chem. 2022 Dec 15. DOI:10.1021/acs.jmedchem.2c00857
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