AS057278
Based on 1 Customer Validation
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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- Purity: 99.76%
- CAS No.: 402-61-9
- 화학식: C5H6N2O2
- 분자량:126.11
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Metabolism/Protease Compound Library
HY-L012
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CNS-Penetrant Compound Library
HY-L028
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Orally Active Compound Library
HY-L061
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Human Metabolite Library
HY-L123
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Heterocyclic Compound Library
HY-L138
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Amino Acid Metabolism Compound Library
HY-L189
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High-Throughput Bioactive Compound Library
HY-L205
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MCE Kinase Hinge Binder Fragment Library
HY-L907
All Amino Acid Oxidase Isoforms
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Biological Activity
IC50: 0.91 μM (DAAO)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Adipocyte | EC50 |
1.4 μM
Compound: 3a
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Inhibition of isoproterenol-induced lipolysis in human subcutaneous adipocytes after 5 hrs
Inhibition of isoproterenol-induced lipolysis in human subcutaneous adipocytes after 5 hrs
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[PMID: 17452318] |
| CHO-K1 | EC50 |
900 nM
Compound: 3a
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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
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[PMID: 17452318] |
| CHO-K1 | IC50 |
434 μM
Compound: 3a
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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
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[PMID: 17452318] |
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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Males C57BL/6J mice[1]
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Dosage:80 mg/kg, 20 mg/kg
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Administration:PO; 20 mg/kg b.i.d for 28 days; 80 mg/kg single dosage
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Result:Normalized phencyclidine (PCP)-induced prepulse inhibition after acute (80 mg/kg) and chronic (20 mg/kg b.i.d.) oral administration in mice.
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Animal Model:Male Sprague-Dawley rats[1]
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Dosage:10 mg/kg
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Administration:PO and IV; single dosage (Pharmacokinetics Analysis)
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Result:Exhibited good pharmacokinetic effect.
Chemical Information
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CAS No. 402-61-9
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Appearance Solid
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분자량 126.11
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화학식 C5H6N2O2
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Color Light yellow to light brown
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SMILES
O=C(C1=NNC(C)=C1)O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (277 KB)
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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)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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.
| 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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