Cat. No. 0571
Chemical Name: 1,4-Dihydro-2,4,6-trimethyl-3,5-pyr
Biological ActivityA 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.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
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.
If you know of a relevant reference for PCA 4248 please let us know.
Citations are publications that use Tocris products. Selected citations for PCA 4248 include:
Hergott et al (2015) Bacterial exploitation of phosphorylcholine mimicry suppresses inflammation to promote airway infection. Mediators Inflamm 125 3878. PMID: 26426079.
Bachi et al (2012) Apoptotic cells contribute to melanoma progression and this effect is partially mediated by the platelet-activating factor receptor. J Pharmacol Exp Ther 2012 610371. PMID: 22577252.
Garcia et al (2010) Platelet-activating factor receptor plays a role in lung injury and death caused by Influenza A in mice. PLoS Pathog 6 e1001171. PMID: 21079759.
Mathison et al (2004) Effects of cannabinoid receptor-2 activation on accelerated gastrointestinal transit in lipopolysaccharide-treated rats. Br J Pharmacol 142 1247. PMID: 15249429.
View Related Products by Target
View Related Products by Product Action
Keywords: PCA 4248, supplier, PAF, receptor, antagonists, Receptors, Platelet-activating, Factor, PCA4248, Tocris Bioscience, Platelet-Activating Factor (PAF) Receptor Antagonist products
Find multiple products by catalog number
New Products in this Area
Highly potent GPR183 (EBI2) agonistAR-C 69931 tetrasodium salt
Highly potent P2Y12 antagonistFTY 720
Potent S1P receptor agonist; also immunosuppressantCinacalcet hydrochloride
Calcium-sensing receptor (CaSR) allosteric agonist; also CYP2D2 inhibitor and Ca2+ channel blocker; orally bioavailableAMG 837 hemicalcium salt
Potent free fatty acid receptor 1 (FFA1/GPR40) partial agonistUMB 68
GHB receptor ligandAZD 1283
High affinity P2Y12 antagonistEx 26
Potent and selective S1P1 receptor antagonist
Follow Tocris on LinkedIn
Visit our LinkedIn page for the latest Tocris news, events and updates.