产品
编 号：F762451
分子式：C18H23NO3
分子量：301.38
分子式：C18H23NO3
分子量：301.38
产品类型
规格
价格
是否有货
结构图
CAS No: 2454459-87-9
产品详情
生物活性：
hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research. hMAO-B-IN-2 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
hMAO-B-IN-2 (compound 6j) (Sprague-Dawley rats; 3 mg/kg, IV; 10 mg/kg, PO; once) has acceptable pharmacokinetic properties.Pharmacokinetic Parameters of hMAO-B-IN-2 in male Sprague-Dawley rats.ParametersIV (3 mg/kg) PO (10 mg/kg)
T1/2 (h)1.02 ± 0.171.33 ± 0.16
Tmax (h)0.3
Cmax (μg/L)639.29 ± 89.06142.17 ± 72.21
AUC0-inf (μg/L?h)247.74 ± 11.48268.49 ± 69.72
CL (L/h/kg)3.33 ± 0.15
F (%)36.10%
Animal Model:Sprague-Dawley rats (male, 220±20 g)
Dosage:3 mg/kg (IV), 10 mg/kg (PO)
Administration:IV, PO (Pharmacokinetic Analysis)
Result:Had acceptable pharmacokinetic properties, and showed a high maximal concentration, appropriate half-life, and good oral bioavailability.
体外研究：
hMAO-B-IN-2 (compound 6j) (0-100 μM, 15 min) exhibits potent inhibitory activity, with IC50 values of 4 nM (hMAO-B) and 6.04 nM (hMAO-A), respectively.hMAO-B-IN-2 (30 min) is a reversible MAO-B inhibitor, the activity of MAO-B enzyme was restored to about 82% and 45% after compound 6j dilution to 0.1 × IC50 and 1 × 50, respectively.hMAO-B-IN-2 (25 μM, 48 h) exhibits remarkable inhibitory activities against MAO-B, had good inhibition property of Aβ self-induce aggregation (40.78 ± 6.27%).hMAO-B-IN-2 (0-100 μM, 24 h) shows non-toxic at the concentrations of 25 μM.hMAO-B-IN-2 (0-25 μM, 24 h) has neuroprotective capability against neurodegeneration disease, and increases cell survival rates in a dose-dependent manner.
hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research. hMAO-B-IN-2 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
hMAO-B-IN-2 (compound 6j) (Sprague-Dawley rats; 3 mg/kg, IV; 10 mg/kg, PO; once) has acceptable pharmacokinetic properties.Pharmacokinetic Parameters of hMAO-B-IN-2 in male Sprague-Dawley rats.ParametersIV (3 mg/kg) PO (10 mg/kg)
T1/2 (h)1.02 ± 0.171.33 ± 0.16
Tmax (h)0.3
Cmax (μg/L)639.29 ± 89.06142.17 ± 72.21
AUC0-inf (μg/L?h)247.74 ± 11.48268.49 ± 69.72
CL (L/h/kg)3.33 ± 0.15
F (%)36.10%
Animal Model:Sprague-Dawley rats (male, 220±20 g)
Dosage:3 mg/kg (IV), 10 mg/kg (PO)
Administration:IV, PO (Pharmacokinetic Analysis)
Result:Had acceptable pharmacokinetic properties, and showed a high maximal concentration, appropriate half-life, and good oral bioavailability.
体外研究：
hMAO-B-IN-2 (compound 6j) (0-100 μM, 15 min) exhibits potent inhibitory activity, with IC50 values of 4 nM (hMAO-B) and 6.04 nM (hMAO-A), respectively.hMAO-B-IN-2 (30 min) is a reversible MAO-B inhibitor, the activity of MAO-B enzyme was restored to about 82% and 45% after compound 6j dilution to 0.1 × IC50 and 1 × 50, respectively.hMAO-B-IN-2 (25 μM, 48 h) exhibits remarkable inhibitory activities against MAO-B, had good inhibition property of Aβ self-induce aggregation (40.78 ± 6.27%).hMAO-B-IN-2 (0-100 μM, 24 h) shows non-toxic at the concentrations of 25 μM.hMAO-B-IN-2 (0-25 μM, 24 h) has neuroprotective capability against neurodegeneration disease, and increases cell survival rates in a dose-dependent manner.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备