Biological Activity
A specific PAF antagonist, more potent than the ginkolide BN-52021. Inhibits rabbit platelet aggregation with an IC50 value of 1.05 μM and has no significant activity on Ca2+ channels. Active in vivo, antagonizing PAF-induced systemic hypotension and protein-plasma extravasation in rats.
Compound Libraries
PCA 4248 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 361.46 |
| Formula | C19H23NO4S |
| Storage | Desiccate at -20°C |
| Purity | ≥95% |
| CAS Number | 123875-01-4 |
| PubChem ID | 4698 |
| InChI Key | DHCNAWNKZMNTIS-UHFFFAOYSA-N |
| Smiles | COC(=O)C1=C(C)NC(C)=C(C1C)C(=O)OCCSC1=CC=CC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 36.14 | 100 | |
| ethanol | 36.14 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 361.46. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 2.77 mL | 13.83 mL | 27.67 mL |
| 5 mM | 0.55 mL | 2.77 mL | 5.53 mL |
| 10 mM | 0.28 mL | 1.38 mL | 2.77 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.55 mL |
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References
References are publications that support the products' biological activity.
Fernandez-Gallardo et al (1990) Pharmacological actions of PCA 4248, a new platelet-activating factor receptor antagonist: in vivo studies. J.Pharmacol.Exp.Ther. 255 34 PMID: 2170626
Sunkel et al (1990) 4-Alkyl-1,4-dihydropyridine derivatives as specific PAF-acether antagonists. J.Med.Chem. 33 3205 PMID: 2175357
Sunkel et al (1990) 1,4-Dihydropyridines, a new class of platelet activating factor receptor antagonists: in vitro pharmacological studies. J.Pharmacol.Exp.Ther. 255 28 PMID: 2170624
Keywords: PCA 4248, supplier, PAF, receptor, antagonists, Receptors, Platelet-activating, Factor, PCA4248, Platelet-activating, Factor, (PAF), Receptors, Platelet-activating, Factor, (PAF), Receptors, Tocris Bioscience
