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Submit ReviewGR 144053 trihydrochloride
Description: Glycoprotein IIb/IIIa (integrin αIIbβ3) receptor antagonist. Antithrombotic
Chemical Name: 4-[4-[4-(Aminoiminomethyl)phenyl]-1-piperazinyl]-1-piperidineacetic acid trihydrochloride
Purity: ≥99% (HPLC)
Biological Activity
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 |
| 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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 45.48 | 100 |
Preparing Stock Solutions
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 |
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Product Datasheets
References
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.
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