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Cangrelor tetrasodium

Names

[ CAS No. ]:
163706-36-3

[ Name ]:
Cangrelor tetrasodium

[Synonym ]:
Tetrasodium 5'-O-[({[dichloro(phosphonato)methyl]phosphinato}oxy)phosphinato]-N-[2-(methylsulfanyl)ethyl]-2-[(3,3,3-trifluoropropyl)sulfanyl]adenosine
Cangrelor tetrasodium
Adenosine, 5'-O-[[[(dichlorophosphonomethyl)hydroxyphosphinyl]oxy]hydroxyphosphinyl]-N-[2-(methylthio)ethyl]-2-[(3,3,3-trifluoropropyl)thio]-, sodium salt (1:4)
UNII-2144G00Y7W
Cangrelor tetrasodium (USAN)

Biological Activity

[Description]:

Cangrelor tetrasodium, an adenosine triphosphate analogue, is a reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor tetrasodium directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor tetrasodium 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

[In Vitro]

Cangrelor tetrasodium is the only potent intravenous direct and specific adenosine diphosphate (ADP) P2Y12 receptor antagonist[1]. 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

[ Boiling Point ]:
979ºC at 760 mmHg

[ Molecular Formula ]:
C17H21Cl2F3N5Na4O12P3S2

[ Molecular Weight ]:
864.286

[ Flash Point ]:
545.9ºC

[ Exact Mass ]:
862.876099

[ PSA ]:
347.26000

[ LogP ]:
4.67630

[ Vapour Pressure ]:
0mmHg at 25°C

[ Storage condition ]:
-20℃

Related Compounds