|(二氯((((((2R,3S,4R,5R)-3,4-3,4-二羟基-5-(6-((2-甲基硫代)乙基)氨基)-2-((3,3,3-三氟丙基)硫代)-9H-嘌呤-9-基)四氢呋喃-2-基)甲氧基)(羟基)磷酰)氧基)(羟基)磷酰)甲基)膦酸四钠盐|CsnPharm

CAS No.: 163706-36-3

Cangrelor tetrasodium Catalog No. CSN22574

Synonyms: AR-C69931MX tetrasodium;AR-C69931MX;Cangrelor sodium salt

Cangrelor is a potent and competitive P2Y12 receptor inhibitor that inhibits of ADP-induced platelet aggregation.

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技术信息

生物活性

描述Cangrelor is the only currently available intravenous platelet P2Y12 receptor inhibitor, and its quick onset and offset make it an appealing option for antiplatelet therapy{[De Luca L, Steg PG, Bhatt DL, Capodanno D, Angiolillo DJ. Cangrelor: Clinical Data, Contemporary Use, and Future Perspectives. J Am Heart Assoc. 2021;10(13):e022125. |https://pubmed.ncbi.nlm.nih.gov/34212768/]}^[1]. In vitro, the experiment focused on αIIbβ3 complex (platelet receptor for fibrinogen), and cangrelor (140μM, 15 min) suppressed the expression of this surface membrane activation marker in platelets^[2]. Cangrelor tetrasodium (10 mg/kg) not only significantly decreases BLM-induced release of inflammatory cytokines (PF4, CD40 L and MPO), but also decreases the increment of platelets, neutrophils and platelet-neutrophil aggregates in the fibrotic lung and in the peripheral blood of BLM-treated mice^[3].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03182855	Acute Coronary Syndrome ... more >> Myocardial Infarction STEMI - ST Elevation Myocardial Infarction Collapse <<	Phase 4	Not yet recruiting	August 1, 2019	Denmark ... more >> Aarhus University Hospital Not yet recruiting Aarhus, Denmark, 8200 Contact: Jacob Thorsted Sorensen, MD, PhD +4540143563 jacsoe@rm.dk Contact: Steen D Kristensen, MD, DMSc +4530922336 stekrist@rm.dk Collapse <<

参考文献

[1] Sible AM, Nawarskas JJ. Cangrelor: A New Route for P2Y12 Inhibition. Cardiol Rev. 2017;25(3):133-139.
[2] Kassassir H, Siewiera K, Sychowski R, Watała C. Can the antiplatelet effects of cangrelor be reliably studied in mice under in vivo and in vitro conditions using flow cytometry?. Pharmacol Rep. 2013;65(4):870-883.
[3] Zhan T, Wei T, Dong L, et al. Cangrelor alleviates bleomycin-induced pulmonary fibrosis by inhibiting platelet activation in mice. Mol Immunol. 2020;120:83-92.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.1570 mL
- 5.7851 mL
- 11.5702 mL
- 5 mM
- 0.2314 mL
- 1.1570 mL
- 2.3140 mL
- 10 mM
- 0.1157 mL
- 0.5785 mL
- 1.1570 mL

技术信息

CAS号

163706-36-3

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H21Cl2F3N5Na4O12P3S2

运输

蓝冰

分子量

864.29

别名

AR-C69931MX tetrasodium;AR-C69931MX;Cangrelor sodium salt;AR-C 69931 Tetrasodium;Cangrelor (sodium salt);AR-C69931;Cangrelor

溶解度

DMSO	2.0 mg/mL (2.3 mM)
Ethanol	Insoluble

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