Cangrelor

Names

[ Name ]:
Cangrelor

[Synonym ]:
UNII-6AQ1Y404U7
Cangrelor
AR-C69931

Biological Activity

[Description]:

Cangrelor (AR-C69931MX), an adenosine triphosphate analogue, is an intravenous, reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor is also a nonspecific GPR17 antagonist[1][2].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> P2Y Receptor

Research Areas >> Inflammation/Immunology

[Target]

P2Y12

[In Vitro]

Cangrelor tetrasodium has pKb of 8.6-9.2 for hP2Y12 receptor[3].

[In Vivo]

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[2].

[References]

[1]. Bhattad VB, , et al. Intravenous cangrelor as a peri-procedural bridge with applied uses in ischemic events. Ann Transl Med. 2019;7(17):408.

[2]. Zhan T, Wei T, et al. Cangrelor alleviates bleomycin-induced pulmonary fibrosis by inhibiting platelet activation in mice. Mol Immunol. 2020;120:83-92.

[3]. Bekő K, et al. Contribution of platelet P2Y12 receptors to chronic Complete Freund's adjuvant-induced inflammatory pain. J Thromb Haemost. 2017;15(6):1223-1235.

Chemical & Physical Properties

[ Density]:
2.087g/cm3

[ Boiling Point ]:
979.004ºC at 760 mmHg

[ Molecular Formula ]:
C₁₇H₂₅Cl₂F₃N₅O₁₂P₃S₂

[ Molecular Weight ]:
776.35900

[ Flash Point ]:
545.882ºC

[ Exact Mass ]:
774.94800

[ PSA ]:
335.94000

[ LogP ]:
2.92350

[ Vapour Pressure ]:
0mmHg at 25°C

[ Index of Refraction ]:
1.722

Related Compounds

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