| 名稱 | Ticagrelor |
| 描述 | Ticagrelor (AR-C 126532XX), produced by AstraZeneca, is an inhibitor of platelet aggregation. Unlike clopidogrel, ticagrelor is not a prodrug required metabolic activation. The drug was approved for use in the European Union by the European Commission on December 3, 2010, and by the US FDA on July 20, 2011. Its trade names are Brilinta (US), Brilique(EU) and Possia(EU). |
| 體外活性 | Ticagrelor的t1/2大約為7-8.5小時.Ticagrelor與血小板聚集的抑制劑量有關(guān),以100-400 mg處理2小時可完全抑制.Ticagrelor有良好的耐受性,既無嚴(yán)重的不良事件,也無明顯的實驗值變化.Ticagrelor吸收快,1.3-2小時即可達(dá)峰.在所研究的劑量范圍內(nèi),Ticagrelor峰值濃度和藥時曲線下面積（從時間0到無窮大的）以明顯的劑量比例增加,表明其線性藥物動力學(xué)特征. |
| 體內(nèi)活性 | 在對rh-P2Y12受體轉(zhuǎn)染的CHO-K1進(jìn)行結(jié)合研究中,Ticagrelor表現(xiàn)出高效可逆的結(jié)合,kon(結(jié)合常數(shù))為0.00011/(nM·s),Kd為10.5 nM,koff(解離常數(shù))為0.00087/s,結(jié)合與解離半衰期值分別為4分鐘和14分鐘,表明可結(jié)合血小板的藥物濃度決定了血小板的抑制大小。Ticagrelor是不需要代謝活化的活性藥物。Ticagrelor不與ADP在ADP結(jié)合位點直接競爭,但會占據(jù)鄰近的結(jié)合位點,改變結(jié)合位點構(gòu)象導(dǎo)致一個可逆的受體的構(gòu)象變化。Ticagrelor與受體結(jié)合是可逆的,快速起/失效。 |
| 存儲條件 | Store under nitrogen,Keep away from direct sunlight,
Pure form: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 250 mg/mL (478.4 mM), Sonication is recommended.
5% DMSO+40 % PEG300+5 % Tween 80+50 % Saline : 5 mg/mL (9.57 mM), Solution.
10% DMSO+90% Saline : < 10 mg/mL (19.14 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (19.14 mM), Solution.
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| 關(guān)鍵字 | Ticagrelor | P2YReceptor | P2Y12 | P2Y Receptor | P2Y | Inhibitor | inhibit | CYP2C9 | AZD-6140 | AZD 6140 |
| 相關(guān)產(chǎn)品 | Naringin | Musk ketone | Ipriflavone | Benzyl alcohol | Clarithromycin | Tauroursodeoxycholate | Memantine hydrochloride | Sudan IV | Naringin dihydrochalcone | Naringenin | Dibenzothiophene | Oxadiazon |
| 相關(guān)庫 | 抑制劑庫 | 抗癌上市藥物庫 | 已知活性化合物庫 | 臨床失敗化合物庫 | EMA 上市藥物庫 | FDA 上市藥物庫 | GPCR靶點分子庫 | 膜蛋白靶向化合物庫 | 神經(jīng)退行性疾病化合物庫 | 免疫/炎癥分子化合物庫 | 藥物功能重定位化合物庫 | 抗癌臨床化合物庫 |