产品
编 号：F754611
分子式：C26H34N2O5S
分子量：486.62
分子式：C26H34N2O5S
分子量：486.62
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CAS No: 2685786-28-9
产品详情
生物活性：
Neuraminidase-IN-11 (15e) is a potent and selective neuraminidase (NA) inhibitor with the IC50 values of 4.7 nM, 8.46 nM and 1.5 nM against H1N1, H5N1 and H5N8 NAs respectively.
体内研究：
Neuraminidase-IN-11 (15e) (oral administration, 50 mg/kg, every second day, 14 days) shows no significant change in body weight and no other toxic side effects in kunming mice.Animal Model:Male Sprague?Dawley rat
Dosage:
Administration:2 mg/kg, i.v.; 20 mg/kg, p.o.
Result:The pharmacokinetic parameters of Neuraminidase-IN-11 (15e)Parameters15e (i.v.)15e (p.o.)
t1/2 (h)0.2130.863
Tmax (h)0.0830.5
Cmax (ng/mL)7195491
Vdss (mL/kg)179-
CL17.2-
F (%)-1.58
体外研究：
Neuraminidase-IN-11 (15e) (0-6 μM, 40 min)has anti-NA (Neuraminidase) activity against H1N1-H274Y mutant and H5N1-H274Y mutant with the IC50 values of 1.07 μM and 0.61 μM, respectively.Neuraminidase-IN-11 (15e) (0-20 μM, 48 h) inhibits chicken embryo fibroblasts (CEFs) infected H5N1 or H5N8 with the IC50 values of 4.4 μM and 0.57 μM respectively, and inhibits Madin?Darby canine kidney (MDCK) cells infected H1N1 or H3N2 with the IC50 values of 0.05 μM and 12.65 μM respectively.Neuraminidase-IN-11 (15e) has no significant inhibitory effect on the major CYP enzymes which acts on CYP1A2, CYP2C9 and CYP2C19 with the IC50 values of 28.9 μM, 47.3 μM and 47.8 μM, respectively.The metabolic stability parameters of Neuraminidase-IN-11 (15e) in human liver microsomes (HLM). ParametersNeuraminidase-IN-11 (15e)
t1/2 (min)>145
CLint(mic) (μL/min/kg) Neuraminidase-IN-11 相关抗体:
Neuraminidase-IN-11 (15e) is a potent and selective neuraminidase (NA) inhibitor with the IC50 values of 4.7 nM, 8.46 nM and 1.5 nM against H1N1, H5N1 and H5N8 NAs respectively.
体内研究：
Neuraminidase-IN-11 (15e) (oral administration, 50 mg/kg, every second day, 14 days) shows no significant change in body weight and no other toxic side effects in kunming mice.Animal Model:Male Sprague?Dawley rat
Dosage:
Administration:2 mg/kg, i.v.; 20 mg/kg, p.o.
Result:The pharmacokinetic parameters of Neuraminidase-IN-11 (15e)Parameters15e (i.v.)15e (p.o.)
t1/2 (h)0.2130.863
Tmax (h)0.0830.5
Cmax (ng/mL)7195491
Vdss (mL/kg)179-
CL17.2-
F (%)-1.58
体外研究：
Neuraminidase-IN-11 (15e) (0-6 μM, 40 min)has anti-NA (Neuraminidase) activity against H1N1-H274Y mutant and H5N1-H274Y mutant with the IC50 values of 1.07 μM and 0.61 μM, respectively.Neuraminidase-IN-11 (15e) (0-20 μM, 48 h) inhibits chicken embryo fibroblasts (CEFs) infected H5N1 or H5N8 with the IC50 values of 4.4 μM and 0.57 μM respectively, and inhibits Madin?Darby canine kidney (MDCK) cells infected H1N1 or H3N2 with the IC50 values of 0.05 μM and 12.65 μM respectively.Neuraminidase-IN-11 (15e) has no significant inhibitory effect on the major CYP enzymes which acts on CYP1A2, CYP2C9 and CYP2C19 with the IC50 values of 28.9 μM, 47.3 μM and 47.8 μM, respectively.The metabolic stability parameters of Neuraminidase-IN-11 (15e) in human liver microsomes (HLM). ParametersNeuraminidase-IN-11 (15e)
t1/2 (min)>145
CLint(mic) (μL/min/kg) Neuraminidase-IN-11 相关抗体:
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