Art. -Nr.: HY-33009

AS057278

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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.

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Reinheit: 99.76%
CAS. Nr.: 402-61-9
Formel: C₅H₆N₂O₂
Molecular Weight:126.11

Speicherung:

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

AS057278 Chemical Structure

CAS. Nr.: 402-61-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC₅₀: 0.91 μM (DAAO)^[1]

Alle Amino Acid Oxidase Isoform-spezifische Produkte anzeigen :

D-Amino acid oxidase

Cellular Effect

Cell Line	Type	Value	Description	References
Adipocyte	EC₅₀	1.4 μM Compound: 3a	Inhibition of isoproterenol-induced lipolysis in human subcutaneous adipocytes after 5 hrs Inhibition of isoproterenol-induced lipolysis in human subcutaneous adipocytes after 5 hrs	[PMID: 17452318]
CHO-K1	EC₅₀	900 nM Compound: 3a	Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA	[PMID: 17452318]
CHO-K1	IC₅₀	434 μM Compound: 3a	Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay	[PMID: 17452318]

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
C_max (ng/mL)	73,559.8	8088.8
t_max (h)	0.083	1
C_Z (ng/mL)	26.8	40.5
t_Z (h)	24	24
AUC_Z (ng/mL·h)	45,596.2	18,254.4
λ_Z (h^-1)	0.124	0.096
AUC (ng/mL·h)	45,810.9	18,649.9
V_Z (L/kg)	1.76
V_SS (L/kg)	0.24
CL (L/kg/h)	0.22
MRT (h)	1.087
F		0.407

MedChemExpress (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.

Chemical Information

CAS. Nr. 402-61-9
Appearance Solid
Molecular Weight 126.11
Formel C₅H₆N₂O₂
Color Light yellow to light brown
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (792.96 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

7.9296 mL

39.6479 mL

79.2959 mL

5 mM

1.5859 mL

7.9296 mL

15.8592 mL

10 mM

0.7930 mL

3.9648 mL

7.9296 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (19.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (19.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (19.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Adage T, et al. In vitro and in vivo pharmacological profile of AS057278, a selective d-amino acid oxidase inhibitor with potential anti-psychotic properties. Eur Neuropsychopharmacol. 2008;18(3):200-214. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	7.9296 mL	39.6479 mL	79.2959 mL	198.2396 mL
	5 mM	1.5859 mL	7.9296 mL	15.8592 mL	39.6479 mL
	10 mM	0.7930 mL	3.9648 mL	7.9296 mL	19.8240 mL
	15 mM	0.5286 mL	2.6432 mL	5.2864 mL	13.2160 mL
	20 mM	0.3965 mL	1.9824 mL	3.9648 mL	9.9120 mL
	25 mM	0.3172 mL	1.5859 mL	3.1718 mL	7.9296 mL
	30 mM	0.2643 mL	1.3216 mL	2.6432 mL	6.6080 mL
	40 mM	0.1982 mL	0.9912 mL	1.9824 mL	4.9560 mL
	50 mM	0.1586 mL	0.7930 mL	1.5859 mL	3.9648 mL
	60 mM	0.1322 mL	0.6608 mL	1.3216 mL	3.3040 mL
	80 mM	0.0991 mL	0.4956 mL	0.9912 mL	2.4780 mL
	100 mM	0.0793 mL	0.3965 mL	0.7930 mL	1.9824 mL

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AS057278

Metabolism/Protease Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Amino Acid Metabolism Compound Library

High-Throughput Bioactive Compound Library

MCE Kinase Hinge Binder Fragment Library

Alle Amino Acid Oxidase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AS057278

Metabolism/Protease Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Amino Acid Metabolism Compound Library

High-Throughput Bioactive Compound Library

MCE Kinase Hinge Binder Fragment Library

Alle Amino Acid Oxidase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AS057278 Related Classifications

HY-33009 Related Classifications