规格 | 价格 | 库存 | 数量 |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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体外研究 (In Vitro) |
体外活性:普拉格雷是一种新型口服活性噻吩并吡啶,比氯吡格雷具有更快、更强和更可靠的血小板聚集抑制作用,反映了其在体内代谢为具有选择性 P2Y(12) 拮抗活性的活性代谢物。
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体内研究 (In Vivo) |
盐酸普拉格雷的活性代谢物的 IC50 值为 1.8 μM,可抑制大鼠血小板中腺苷 ADP(10μM)产生的体外血小板聚集[2]。在体内,盐酸普拉格雷比氯吡格雷表现出更大的效力并且起效更快。盐酸普拉格雷的活性抗血小板代谢物是由无活性前药在体内代谢分解产生的。盐酸普拉格雷从胃中很快被吸收。口服 60 mg 标准负荷剂量后,活性代谢物的血浆浓度在 1 小时内达到最大,1-2 小时内可最大程度地抑制血小板聚集[1]。
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动物实验 |
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毒性/毒理 (Toxicokinetics/TK) |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation No published information is available on the use of prasugrel during breastfeeding. Until more data become available, prasugrel should be used with caution during breastfeeding, especially while nursing a newborn or preterm infant. If it is used by a nursing mother, monitor the infant for bruising and bleeding. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
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参考文献 | |||
其他信息 |
Prasugrel Hydrochloride is the hydrochloride salt form of prasugrel, an orally bioavailable thienopyridine, with antiplatelet activity. Upon oral administration, the active metabolite of prasugrel targets and irreversibly binds to the platelet receptor for adenosine diphosphate (ADP), thereby blocking the binding of ADP to its receptor. This inhibits ADP-mediated activation of the glycoprotein complex GPIIb/IIIa, fibrinogen binding to platelets and platelet adhesion and aggregation. This results in increased bleeding time.
A piperazine derivative and PLATELET AGGREGATION INHIBITOR that is used to prevent THROMBOSIS in patients with ACUTE CORONARY SYNDROME; UNSTABLE ANGINA and MYOCARDIAL INFARCTION, as well as in those undergoing PERCUTANEOUS CORONARY INTERVENTIONS. See also: Prasugrel (has active moiety). |
精确质量 |
409.091
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CAS号 |
389574-19-0
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相关CAS号 |
Prasugrel;150322-43-3;Prasugrel (Maleic acid);389574-20-3;Prasugrel-d5;1127252-92-9
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PubChem CID |
10158453
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外观&性状 |
Light yellow to yellow solid powder
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沸点 |
493.5ºC at 760 mmHg
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闪点 |
252.3℃
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LogP |
4.63
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tPSA |
74.85
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氢键供体(HBD)数目 |
1
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氢键受体(HBA)数目 |
6
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可旋转键数目(RBC) |
6
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重原子数目 |
27
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分子复杂度/Complexity |
555
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定义原子立体中心数目 |
0
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SMILES |
FC1=CC=CC=C1C(C(C2CC2)=O)N3CCC4=C(C3)C=C(S4)OC(C)=O.Cl
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InChi Key |
JALHGCPDPSNJNY-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C20H20FNO3S.ClH/c1-12(23)25-18-10-14-11-22(9-8-17(14)26-18)19(20(24)13-6-7-13)15-4-2-3-5-16(15)21;/h2-5,10,13,19H,6-9,11H2,1H3;1H
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化学名 |
Ethanone, 2-(2-(acetyloxy)-6,7-dihydrothieno(3,2-c)pyridin-5(4H)-yl)-1-cyclopropyl-2-(2-fluorophenyl)-, hydrochloride
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别名 |
Prasugrel HydrochloridePrasugrel HClCS-747CS747CS 747PCR-4099PCR4099PCR 4099LY-640315LY640315LY 640315
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month 注意: 请将本产品存放在密封且受保护的环境中(例如氮气保护),避免吸湿/受潮和光照。 |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外实验) |
DMSO : ~41.67 mg/mL (~101.66 mM)
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溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 2.08 mg/mL (5.07 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将100 μL 20.8 mg/mL澄清DMSO储备液加入400 μL PEG300中,混匀;然后向上述溶液中加入50 μL Tween-80,混匀;加入450 μL生理盐水定容至1 mL。 *生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。 配方 2 中的溶解度: ≥ 2.08 mg/mL (5.07 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 例如,若需制备1 mL的工作液,可将 100 μL 20.8 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中,混匀。 *20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。 View More
配方 3 中的溶解度: ≥ 2.08 mg/mL (5.07 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04445623 | UNKNOWN STATUS | Drug: Prasugrel Hydrochloride 10 MG Oral Tablet Drug: Placebo |
COVID19 Thrombosis |
Azienda Ospedaliera Universitaria Integrata Verona | 2020-07 | Phase 3 |
NCT00059215 | COMPLETEDWITH RESULTS | Drug: Prasugrel (CS-747) Drug: Clopidogrel |
Cardiovascular Diseases Heart Diseases |
Eli Lilly and Company | 2003-04 | Phase 2 |
NCT05359224 | RECRUITING | Drug: Prasugrel group Drug: Clopidogrel group |
Intracranial Aneurysm | Yonsei University | 2022-06-13 | Phase 4 |
NCT01852019 | COMPLETEDWITH RESULTS | Drug: Cangrelor Drug: Prasugrel |
Coronary Artery Disease | The Medicines Company | 2013-06 | Phase 2 |
NCT02212028 | COMPLETEDWITH RESULTS | Drug: prasugrel | Coronary Artery Disease | University of Florida | 2014-10 | Phase 4 |