产品
编 号：F349107
分子式：C5H6N2O2
分子量：126.11
分子式：C5H6N2O2
分子量：126.11
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
288
In-stock
5mg
720
In-stock
10mg
1120
In-stock
结构图
CAS No: 402-61-9
产品详情
生物活性：
AS057278 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant non-peptidic D-amino acid oxidase (DAAO) inhibitor with an IC50 value of 0.91 μM and EC50 of 2.2-3.95 μM. AS057278 can normalize phencyclidine (PCP)-induced prepulse inhibition in mice. AS057278 can be used for researching schizophrenia.
体内研究：
AS057278 (PO; 20 mg/kg b.i.d for 28 days; 80 mg/kg single dosage) normalizes?phencyclidine?(PCP)-induced?prepulse inhibition.AS057278 (10 mg/kg; PO and IV; single dosage) exhibits good pharmacokinetic effects.Pharmacokinetic Parameters of AS057278 in male Sprague-Dawley rats.IV (10 mg/kg) PO (10 mg/kg)
C0 (ng/mL)100,557.3
Cmax (ng/mL)73,559.88088.8
tmax (h)0.0831
CZ (ng/mL)26.840.5
tZ (h)2424
AUCZ (ng/mL·h)45,596.218,254.4
λZ (h^-1)0.1240.096
AUC (ng/mL·h)45,810.918,649.9
VZ (L/kg)1.76
VSS (L/kg)0.24
CL (L/kg/h)0.22
MRT (h)1.087
F0.407
Animal Model:Males C57BL/6J mice
Dosage:80 mg/kg, 20 mg/kg
Administration:PO; 20 mg/kg b.i.d for 28 days; 80 mg/kg single dosage
Result:Normalized?phencyclidine?(PCP)-induced?prepulse inhibition?after acute (80?mg/kg) and chronic (20?mg/kg b.i.d.)?oral administration?in mice.
Animal Model:Male Sprague-Dawley rats
Dosage:10 mg/kg
Administration:PO and IV; single dosage (Pharmacokinetics Analysis)
Result:Exhibited good pharmacokinetic effect.
AS057278 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant non-peptidic D-amino acid oxidase (DAAO) inhibitor with an IC50 value of 0.91 μM and EC50 of 2.2-3.95 μM. AS057278 can normalize phencyclidine (PCP)-induced prepulse inhibition in mice. AS057278 can be used for researching schizophrenia.
体内研究：
AS057278 (PO; 20 mg/kg b.i.d for 28 days; 80 mg/kg single dosage) normalizes?phencyclidine?(PCP)-induced?prepulse inhibition.AS057278 (10 mg/kg; PO and IV; single dosage) exhibits good pharmacokinetic effects.Pharmacokinetic Parameters of AS057278 in male Sprague-Dawley rats.IV (10 mg/kg) PO (10 mg/kg)
C0 (ng/mL)100,557.3
Cmax (ng/mL)73,559.88088.8
tmax (h)0.0831
CZ (ng/mL)26.840.5
tZ (h)2424
AUCZ (ng/mL·h)45,596.218,254.4
λZ (h^-1)0.1240.096
AUC (ng/mL·h)45,810.918,649.9
VZ (L/kg)1.76
VSS (L/kg)0.24
CL (L/kg/h)0.22
MRT (h)1.087
F0.407
Animal Model:Males C57BL/6J mice
Dosage:80 mg/kg, 20 mg/kg
Administration:PO; 20 mg/kg b.i.d for 28 days; 80 mg/kg single dosage
Result:Normalized?phencyclidine?(PCP)-induced?prepulse inhibition?after acute (80?mg/kg) and chronic (20?mg/kg b.i.d.)?oral administration?in mice.
Animal Model:Male Sprague-Dawley rats
Dosage:10 mg/kg
Administration:PO and IV; single dosage (Pharmacokinetics Analysis)
Result:Exhibited good pharmacokinetic effect.
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