[CAS NO. 919351-41-0] AZD1283
PRODUCTS SPECIFICATIONS [919351-41-0]
DESCRIPTION [919351-41-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 470.54 |
| Molecular Formula | C23H26N4O5S |
| SMILES | CC1=C(C(OCC)=O)C=C(C#N)C(N2CCC(C(NS(=O)(CC3=CC=CC=C3)=O)=O)CC2)=N1 |
Summary
IC50 & Target
|
P2Y12 Receptor 11 nM (IC 50 ) |
In Vitro
AZD1283 exhibits excellent antiplatelet aggregation potency with an IC
50
value of 3.6 μM
[1]
.
AZD1283 has highly inhibitory activity against CYP450 with IC
50
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
EC
50
value of 3 μg/(kg×min)
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AZD1283 exhibits poor liver microsomal stability in rat (T
1/2
= 6.08 min), but better in dog microsomes (T
1/2
= 201 min) and human microsomes (T
1/2
= 65.0 min)
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Sprague-Dawley rats [1] |
| Dosage: | 5 mg/kg |
| Administration: | p.o.; single dosage |
| Result: | Exhibited a C max of 25.9 ± 11 ng/mL, a T 1/2 of 1.68 ± 0.37 h and a T max of 0.25 h. |
Appearance
Solid
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 |
Solvent & Solubility
DMSO : 100 mg/mL ( 212.52 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1252 mL | 10.6261 mL | 21.2522 mL |
| 5 mM | 0.4250 mL | 2.1252 mL | 4.2504 mL |
| 10 mM | 0.2125 mL | 1.0626 mL | 2.1252 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.31 mM); Clear solution
References
- [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):
- [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.