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Chemical Structure| 163706-36-3 Chemical Structure| 163706-36-3

Structure of Cangrelor tetrasodium
CAS No.: 163706-36-3

Chemical Structure| 163706-36-3

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

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

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Product Details of Cangrelor tetrasodium

CAS No. :163706-36-3
Formula : C17H21Cl2F3N5Na4O12P3S2
M.W : 864.29
SMILES Code : O=P(C(Cl)(P([O-])([O-])=O)Cl)(OP([O-])(OC[C@H]1O[C@@H](N2C=NC3=C(NCCSC)N=C(SCCC(F)(F)F)N=C23)[C@H](O)[C@@H]1O)=O)[O-].[Na+].[Na+].[Na+].[Na+]
Synonyms :
AR-C69931MX tetrasodium; Cangrelor (sodium salt); AR-C69931MX
MDL No. :MFCD14635359
InChI Key :COWWROCHWNGJHQ-OPKBHZIBSA-J
Pubchem ID :10260031

Safety of Cangrelor tetrasodium

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Cangrelor tetrasodium

GPCR

Isoform Comparison

Biological Activity

Target
  • P2Y receptor

In Vitro:

Cell Line
Concentration Treated Time Description References
BV-2 cells 20, 40, 80 μM 24 hours To evaluate the inhibitory effect of Cangrelor on LPS-induced inflammatory response in BV-2 cells. Results showed that Cangrelor significantly inhibited LPS-induced release of TNF-α, IL-1β, and IL-6, downregulated NF-κB p65 expression, and upregulated p-CREB and BDNF expression. PMC10662506
BLA glutamatergic neurons 100 nmol/L Cangrelor inhibition of GPR17 reversed the CRS-induced increase in firing rate and decrease in rheobase of BLA glutamatergic neurons. PMC11628806
Platelets 200 µM 2 minutes To test the effect of Cangrelor on platelet S1P release, results showed that Cangrelor inhibited S1P release PMC10133218
Murine platelets 100 nM 10 minutes To study the effect of P2Y12 receptor antagonist on platelet aggregation, results showed that Cangrelor significantly inhibited platelet aggregation. PMC3071452
CHO-K1 cells 0.5 ± 0.1 nM 12 minutes To assess the partial agonist effect of AR-C69931MX on P2Y13 receptor, results showed AR-C69931MX as a partial agonist inhibiting cAMP accumulation. PMC11139085
HepG2 cells 100 nM 10 minutes To evaluate the effect of AR-C69931MX on TG-HDL2 internalization, results showed that AR-C69931MX alone increased TG-HDL2 internalization more than ADP. PMC11139085

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice FeCl3-induced carotid artery thrombosis model Intravenous injection 30 μg/kg Single injection Comparison of the antithrombotic effects of M3mP6 HLPN with the intravenous P2Y12 inhibitor cangrelor, showing that cangrelor had similar effects to M3mP6 HLPN in most mice but was more effective in some mice PMC8061427
ICR mice LPS-induced cognitive impairment model Microinjection into hippocampal DG region 2.0 μg and 4.0 μg Daily administration for 3 weeks To evaluate the ameliorative effect of Cangrelor on LPS-induced cognitive impairment in mice. Results showed that Cangrelor pretreatment significantly improved LPS-induced spatial learning and memory deficits, reduced neuroinflammation and oxidative stress, and inhibited hippocampal neuronal apoptosis. PMC10662506
C57BL/6J mice Chronic restraint stress (CRS) model Bilateral BLA injection 0.5 nmol/site, 1 nmol/mouse Once daily for 3 consecutive days Cangrelor significantly ameliorated CRS-induced anxiety-like behaviors in mice, including increased time spent in open arms and entries of open arms, decreased time in closed arms and entries of closed arms in EPM test; increased time in center in OFT; reduced latency to feed in NSF test. PMC11628806
Mice Acute myocardial infarction model Intravenous injection 200 µM Single administration To test the protective effect of Cangrelor on myocardial infarction, results showed that Cangrelor failed to protect the myocardium PMC10133218
Mice Low-density lipoprotein receptor-deficient mice (LDLR−/−) and C57Bl/6 wild-type mice In vitro 100 nM Single dose, lasting 10 minutes To evaluate the effect of Cangrelor on platelet aggregation in hypercholesterolemic mice, results showed that Cangrelor significantly inhibited platelet aggregation. PMC3071452
C57BL/6 mice Ferric chloride-induced thrombosis model Intravenous injection 0.2 mg/kg b.w. Single dose To evaluate the antithrombotic effect of Cangrelor in combination with HE-NECA, results showed that the combination significantly prolonged the time to occlusion and reduced the ratio of total occlusion. PMC8002731

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03182855 Acute Coronary Syndrome ... More >> Myocardial Infarction STEMI - ST Elevation Myocardial Infarction Less << 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 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.16mL

0.23mL

0.12mL

5.79mL

1.16mL

0.58mL

11.57mL

2.31mL

1.16mL

References

 

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