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AZD1283

Catalog No. T3536   CAS 919351-41-0

AZD1283 is an effective P2Y12 receptor antagonist (EC50: 3.0 ug/kg/min, binding IC50: 11 nM). AZD1283 dose-dependently induced increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 and 10 μg/kg/min, respectively. The doses induced the increase in bleeding time at 33 and 100 μg/kg/min for 3- and 13-fold, respectively. Thus, the therapeutic index (TI) was ≥10 for both compounds.

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AZD1283 Chemical Structure
AZD1283, CAS 919351-41-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 31.00
2 mg In stock $ 44.00
5 mg In stock $ 72.00
10 mg In stock $ 126.00
25 mg In stock $ 222.00
50 mg In stock $ 355.00
100 mg In stock $ 592.00
500 mg In stock $ 1,270.00
1 mL * 10 mM (in DMSO) In stock $ 74.00
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Purity: 99.621%
Purity: 98.37%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description AZD1283 is an effective P2Y12 receptor antagonist (EC50: 3.0 ug/kg/min, binding IC50: 11 nM). AZD1283 dose-dependently induced increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 and 10 μg/kg/min, respectively. The doses induced the increase in bleeding time at 33 and 100 μg/kg/min for 3- and 13-fold, respectively. Thus, the therapeutic index (TI) was ≥10 for both compounds.
Targets&IC50 P2Y12 receptor:11 nM
In vivo Acute administration of dasotraline dose-dependently decreases the spontaneous firing rate of LC NE, VTA DA and DR 5-HT neurons through the activation of α2, D2 and 5-HT1A autoreceptors, respectively. Dasotraline predominantly inhibits the firing rate of LC NE neurons while producing only a partial decrease in VTA DA and DR 5-HT neuronal discharge. SEP-225289 is equipotent at inhibiting 5-HT and NE transporters since it prolongs to the same extent the time required for a 50% recovery of the firing activity of dorsal hippocampus CA3 pyramidal neurons from the inhibition induced by microiontophoretic application of 5-HT and NE[1]. Average dopamine and serotonin transporter occupancies increase with increasing doses of SEP-225289. Mean dopamine and serotonin transporter occupancies are 33%±11% and 2%±13%, respectively, for 8 mg; 44%±4% and 9%±10%, respectively, for 12 mg; and 49%±7% and 14%±15%, respectively, for 16 mg[2].
Molecular Weight 470.54
Formula C23H26N4O5S
CAS No. 919351-41-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 22.5 mg/mL (47.82 mM)

TargetMolReferences and Literature

1. 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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-COVID-19 Compound Library Immunology/Inflammation Compound Library Bioactive Compound Library Target-Focused Phenotypic Screening Library Bioactive Compounds Library Max GPCR Compound Library NO PAINS Compound Library Anti-Obesity Compound Library Inhibitor Library Neuronal Signaling Compound Library

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Keywords

AZD1283 919351-41-0 GPCR/G Protein Neuroscience P2Y Receptor thromboembolic antiplatelet aggregation inhibit Inhibitor antithrombotic AZD 1283 AZD-1283 inhibitor

 

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