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Submit ReviewGR 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.
M. Wt | 454.83 |
Formula | C18H27N5O2.3HCl |
Storage | Desiccate at +4°C |
Purity | ≥99% (HPLC) |
CAS Number | 1215333-48-4 |
PubChem ID | 107895 |
InChI Key | GFZHNFOGCMEYTA-UHFFFAOYSA-N |
Smiles | Cl.Cl.Cl.NC(=N)C1=CC=C(C=C1)N1CCN(CC1)C1CCN(CC(O)=O)CC1 |
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
water | 45.48 | 100 |
The following data is based on the product molecular weight 454.83. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.2 mL | 10.99 mL | 21.99 mL |
5 mM | 0.44 mL | 2.2 mL | 4.4 mL |
10 mM | 0.22 mL | 1.1 mL | 2.2 mL |
50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
References are publications that support the biological activity of the product.
Eldred et al (1994) 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. J.Med.Chem. 37 3882 PMID: 7966149
Matsuno et al (1997) 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. Br.J.Pharmacol. 122 1099 PMID: 9480031
Matsuno et al (1999) Comparative antiplatelet effects of aspirin, vapiprost and GR 144053, a GPIIb/IIIa antagonist with special reference to the role of platelet microaggregates. Br.J.Pharmacol. 127 1129 PMID: 10455258
If you know of a relevant reference for GR 144053 trihydrochloride, please let us know.
Keywords: GR 144053 trihydrochloride, GR 144053 trihydrochloride supplier, Glycoprotein, IIb/IIIa, αIIbβ3, alphaIIbβ3, beta3, antagonists, Antithrombotic, receptor, Adhesion, Molecules, Integrin, Receptors, GR144053, trihydrochloride, Cell, Integrins, 1263, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for GR 144053 trihydrochloride include:
Pavlou et al (2023) CRISPR-Cas9 genetic screen leads to the discovery of L-Moses, a KAT2B inhibitor that attenuates Tunicamycin-mediated neuronal cell death. Sci.Rep. 13 3934 PMID: 36894612
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