AZD1283
Based on 1 Customer Validation
AZD1283 is a potent P2Y12 receptor antagonist with a binding IC50 of 11 nM and a GTPγS IC50 of 25 nM. AZD1283 has excellent antiplatelet aggregation potency. AZD1283 can be used to research thromboembolic disorders.
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- Pureza: 99.33%
- No. CAS: 919351-41-0
- Fòrmula: C23H26N4O5S
- Peso molecular:470.54
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Ver todos los productos específicos de isoformas P2Y Receptor
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Actividad biológica
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P2Y12 Receptor 11 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.011 μM
Compound: 3, AZD1283
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Displacement of [125I]-AZ11931285 from P2Y12 receptor (unknown origin) expressed in CHO cell membrane after 1 hr by scintillation counting analysis
Displacement of [125I]-AZ11931285 from P2Y12 receptor (unknown origin) expressed in CHO cell membrane after 1 hr by scintillation counting analysis
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[PMID: 23899349] |
| CHO | IC50 |
0.025 μM
Compound: 3, AZD1283
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Antagonist activity at P2Y12 receptor (unknown origin) expressed in CHO cell membrane by [35S]GTPgammaS binding assay
Antagonist activity at P2Y12 receptor (unknown origin) expressed in CHO cell membrane by [35S]GTPgammaS binding assay
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[PMID: 23899349] |
| CHO-K1 | IC50 |
14 nM
Compound: 1
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Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 60 seconds
Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 60 seconds
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[PMID: 24835983] |
| CHO-K1 | IC50 |
22 nM
Compound: 1
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Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 30 seconds
Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 30 seconds
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[PMID: 24835983] |
| CHO-K1 | IC50 |
44 nM
Compound: 1
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Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 10 seconds
Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 10 seconds
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[PMID: 24835983] |
| CHO-K1 | IC50 |
9 nM
Compound: 1
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Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 60 mins
Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 60 mins
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[PMID: 24835983] |
AZD1283 exhibits excellent antiplatelet aggregation potency with an IC50 value of 3.6 μM[1].
AZD1283 has highly inhibitory activity against CYP450 with IC50 values of 6.62 μM, 0.399 μM and 4.28 μM and 3.64 μM for CYP2C9, CYP2C19, CYP3A4 (Midazolam as the substrate) and CYP3A4 (Testosterone as the substrate), respectively[1].
AZD1283 induces increases in blood flow and inhibition of ADP-induced platelet aggregation with an antithrombotic EC50 value of 3 μg/(kg×min)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats[1]
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Dosage:5 mg/kg
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Administration:p.o.; single dosage
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Result:Exhibited a Cmax of 25.9 ± 11 ng/mL, a T1/2 of 1.68 ± 0.37 h and a Tmax of 0.25 h.
Chemical Information
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No. CAS 919351-41-0
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Appearance Solid
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Peso molecular 470.54
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Fòrmula C23H26N4O5S
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Color White to yellow
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SMILES
CC1=C(C(OCC)=O)C=C(C#N)C(N2CCC(C(NS(=O)(CC3=CC=CC=C3)=O)=O)CC2)=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
DMSO : 100 mg/mL (212.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (5.31 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.
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.
Pureza y Documentación
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Ficha de datos (276 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Kong D, et al. Optimization of P2Y12 Antagonist Ethyl 6-(4-((Benzylsulfonyl)carbamoyl)piperidin-1-yl)-5-cyano-2-methylnicotinate (AZD1283) Led to the Discovery of an Oral Antiplatelet Agent with Improved Druglike Properties. J Med Chem. 2019 Mar 28;62(6):3088-3106. [Content Brief]
[2]. Bach P, et al. Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. J Med Chem. 2013 Sep 12;56(17):7015-24. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1252 mL | 10.6261 mL | 21.2522 mL | 53.1304 mL |
| 5 mM | 0.4250 mL | 2.1252 mL | 4.2504 mL | 10.6261 mL | |
| 10 mM | 0.2125 mL | 1.0626 mL | 2.1252 mL | 5.3130 mL | |
| 15 mM | 0.1417 mL | 0.7084 mL | 1.4168 mL | 3.5420 mL | |
| 20 mM | 0.1063 mL | 0.5313 mL | 1.0626 mL | 2.6565 mL | |
| 25 mM | 0.0850 mL | 0.4250 mL | 0.8501 mL | 2.1252 mL | |
| 30 mM | 0.0708 mL | 0.3542 mL | 0.7084 mL | 1.7710 mL | |
| 40 mM | 0.0531 mL | 0.2657 mL | 0.5313 mL | 1.3283 mL | |
| 50 mM | 0.0425 mL | 0.2125 mL | 0.4250 mL | 1.0626 mL | |
| 60 mM | 0.0354 mL | 0.1771 mL | 0.3542 mL | 0.8855 mL | |
| 80 mM | 0.0266 mL | 0.1328 mL | 0.2657 mL | 0.6641 mL | |
| 100 mM | 0.0213 mL | 0.1063 mL | 0.2125 mL | 0.5313 mL |
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