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AS057278 

Cat. No.: HY-33009
Handling Instructions

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.

For research use only. We do not sell to patients.

AS057278 Chemical Structure

AS057278 Chemical Structure

CAS No. : 402-61-9

Size Price Stock Quantity
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
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100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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[1].

IC50 & Target

IC50: 0.91 μM (DAAO)[1]

In Vivo

AS057278 (PO; 20 mg/kg b.i.d for 28 days; 80 mg/kg single dosage) normalizes phencyclidine (PCP)-induced prepulse inhibition[1].
AS057278 (10 mg/kg; PO and IV; single dosage) exhibits good pharmacokinetic effects[1].
Pharmacokinetic Parameters of AS057278 in male Sprague-Dawley rats[1].

IV (10 mg/kg) PO (10 mg/kg)
C0 (ng/mL) 100,557.3
Cmax (ng/mL) 73,559.8 8088.8
tmax (h) 0.083 1
CZ (ng/mL) 26.8 40.5
tZ (h) 24 24
AUCZ (ng/mL·h) 45,596.2 18,254.4
λZ (h^-1) 0.124 0.096
AUC (ng/mL·h) 45,810.9 18,649.9
VZ (L/kg) 1.76
VSS (L/kg) 0.24
CL (L/kg/h) 0.22
MRT (h) 1.087
F 0.407

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Males C57BL/6J mice[1]
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[1]
Dosage: 10 mg/kg
Administration: PO and IV; single dosage (Pharmacokinetics Analysis)
Result: Exhibited good pharmacokinetic effect.
Molecular Weight

126.11

Formula

C5H6N2O2

CAS No.
SMILES

O=C(C1=NNC(C)=C1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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