GR 144053 trihydrochloride

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1263/10
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GR 144053 trihydrochloride | CAS No. 1215333-48-4 | Integrin Receptor Inhibitors
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Description: Glycoprotein IIb/IIIa (integrin αIIbβ3) receptor antagonist. Antithrombotic

Chemical Name: 4-[4-[4-(Aminoiminomethyl)phenyl]-1-piperazinyl]-1-piperidineacetic acid trihydrochloride

Purity: ≥99%

Product Details
Citations (1)
Reviews

Biological Activity

GR 144053 trihydrochloride is a potent and selective platelet fibrinogen receptor glycoprotein IIb/IIIa (GpIIb/IIIa) antagonist (IC50 = 37 nM). Orally active and highly effective at inhibiting thrombus formation in vivo.

Technical Data

M.Wt:
454.83
Formula:
C18H27N5O2.3HCl
Solubility:
Soluble to 100 mM in water
Purity:
≥99%
Storage:
Desiccate at +4°C
CAS No:
1215333-48-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
    Fox JT, Sakamuru S, Huang R
    Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
  2. GpIbalpha-VWF blockade restores vessel patency by dissolving platelet aggregates formed under very high shear rate in mice.
    Le Behot A, Gauberti M, Martinez De Lizarrondo S, Montagne A, Lemarchand E, Repesse Y, Guillou S, Denis C, Maubert E, Orset C, Vivien D
    Blood, 2014;123(21):3354-63.
  3. Gq pathway regulates proximal C-type lectin-like receptor 2 (CLEC-2) signaling in platelets
    R Badolia, V Inamdar, BK Manne, C Dangelmaie, SP Kunapuli
    J. Biol. Chem., 2017;0(0):.
  4. Orally active non-peptide fibrinogen receptor (GpIIb/IIIa) antagonists: identification of 4-[4-[4-(aminoiminomethyl)phenyl]-1-piperazinyl]-1-piperidineacetic acid as a long-acting, broad spectrum antithrombotic agent.
    Eldred et al.
    J.Med.Chem., 1994;37:3882
  5. GR 144053, a fibrinogen receptor antagonist, enhances the suppression of neointima formation by losartan, an angiotensin II receptor antagonist, in the injured carotid artery of hamster.
    Matsuno et al.
    Br.J.Pharmacol., 1997;122:1099
  6. Comparative antiplatelet effects of aspirin, vapiprost and GR 144053, a GPIIb/IIIa antagonist with special reference to the role of platelet microaggregates.
    Matsuno et al.
    Br.J.Pharmacol., 1999;127:1129
  7. Soluble fibrin causes an acquired platelet glycoprotein VI signaling defect: implications for coagulopathy.
    M Y Lee, C C Verni, B A Herbig, S L Diamond
    Journal of Thrombosis and Haemostasis : Jth, 2017;0(0):1538-7836.
  8. Neutrophils promote venular thrombosis by shaping the rheological environment for platelet aggregation
    D Puhr-Weste, SJ Schink, M Fabritius, L Mittmann, MET Hessenauer, J Pircher, G Zuchtriege, B Uhl, M Holzer, S Massberg, F Krombach, CA Reichel
    Sci Rep, 2019;9(1):15932.

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Citation for GR 144053 trihydrochloride

The citations listed below are publications that use Tocris products. Selected citations for GR 144053 trihydrochloride include:

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