Home Neuronal Signaling P2 Receptor inhibitor Cangrelor Tetrasodium For research use only.

Cangrelor Tetrasodium

Synonyms: AR-C69931MX

Cangrelor (AR-C69931MX) is a potent, competitive P2Y12 receptor inhibitor that is administered by intravenous infusion and rapidly achieves near complete inhibition of ADP-induced platelet aggregation.

Cangrelor Tetrasodium Chemical Structure

Cangrelor Tetrasodium Chemical Structure

CAS No. 163706-36-3

Purity & Quality Control

Cangrelor Tetrasodium Related Products

Signaling Pathway

P2 Receptor Signaling Pathways

P2 Receptor Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
1321N1 Function assay 30 mins Antagonist activity at human GPR17 R255I mutant expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay, IC50=0.00015μM 20394377
1321N1 Function assay 30 mins Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay, IC50=0.0007μM 20394377
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Biological Activity

Description Cangrelor (AR-C69931MX) is a potent, competitive P2Y12 receptor inhibitor that is administered by intravenous infusion and rapidly achieves near complete inhibition of ADP-induced platelet aggregation.
Targets
P2Y12 receptor [1]
In vitro
In vitro Cangrelor is an intravenous ATP analog that directly inhibits, without the need for being metabolized, the P2Y12 receptor in a reversible manner. Cangrelor has a rapid-onset and -offset mechanism of action and achieves significantly greater degrees of platelet inhibition compared with clopidogrel[1].
In Vivo
In vivo Cangrelor is rapidly deactivated by plasmatic ectonucleotidases and, thus, has an extrmely short half-life (2-5 min). Preclinical studies performed in animal models in the early stages of cangrelor development show efficacy in inhibiting thrombus formation and ADP-induced platelet aggregation, as well as a lower increase of bleeding times when compared with IIb/IIIa antagonist[1].

Chemical Information & Solubility

Molecular Weight 864.29 Formula

21Cl2F3N5O12P3S2.4Na
CAS No. 163706-36-3 SDF Download Cangrelor Tetrasodium SDF
Smiles CSCCNC1=C2C(=NC(=N1)SCCC(F)(F)F)N(C=N2)C3C(C(C(O3)COP(=O)([O-])OP(=O)(C(P(=O)([O-])[O-])(Cl)Cl)[O-])O)O.[Na+].[Na+].[Na+].[Na+]
Storage (From the date of receipt)

In vitro
Batch:

Water : 100 mg/mL

DMSO : 2 mg/mL ( (2.31 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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