| AZD1283Potent P2Y12 antagonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.15%
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Chemical structure
| Animal experiment [1]: | |
Animal models | A modified Folts dog model |
Dosage form | 0.1 ~ 33 μg/(kg × min); 5 consecutive 30 min periods |
Applications | AZD1283 dose-dependently increased blood flow and inhibited ADP-induced platelet aggregation with an antithrombotic ED50 value of 3 μg/(kg × min). A dose higher than 33 μg/(kg × min) was required for induction of a larger than 3.5-fold increase in bleeding time. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Bach P, Antonsson T, Bylund R, Bjrkman JA, sterlund K, Giordanetto F, van Giezen JJ, Andersen SM, Zachrisson H, Zetterberg F. 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;56(17):7015-24. | |
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| Cas No. | 919351-41-0 | SDF | Download SDF |
| Formula | C23H26N4O5S | M.Wt | 470.54 |
| Solubility | ≥18.15mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 0.011, 0.025 and 3.2 μM for binding, GTPγS and residual platelet count (RPC), respectively
The central role of the P2Y12 receptor in platelet function makes it an attractive target for the development of novel antiplatelet therapies. AZD1283 is found to be a potent, selective and reversible antagonist of the P2Y12 receptor.
In vitro: It was observed that the benzylic AZD1283 and its analogue 13 were both potent in the higher order residual platelet count assay in which the two tested 5-chlorothienyls showed low (IC50 >22 μM) potency [1].
In vivo: In a modified Folts model in dog, both AZD1283 and its analogue 13 could dose-dependently induce increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 and 10.0 μg/kg/min, respectively. The dose that induced a larger than 3-fold increase in bleeding time were 33 and 100 μg/kg/min for AZD1283 and 13, respectively [2].
Clinical trials: Currenlty there is no clinical data available.
Reference:[1] Bach P, Antonsson T, Bylund R, Björkman JA, Österlund K, Giordanetto F, van Giezen JJ, Andersen SM, Zachrisson H, Zetterberg F. 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;56(17):7015-24.
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将来可能会出现基于免疫方法的试剂盒，不过因为H7N9是个新病毒，爆发至今不足一月，这么快时间还来不及生产抗体，所以目前的检测试剂盒只能是PCR检测试剂盒。
查到了：
4月7日，上海之江生物科技有限公司官方微博称，该公司成功研制禽流感H7N9(2013)核酸测定试剂盒(荧光PCR法)，是针对国内此次H7N9病毒最早研制成功的产品，也是国内目前唯一供应的成品化试剂盒。
