PCA 4248A competitive inhibitor of PAF at the PAF-R level

PCA 4248 (CAS 123875-01-4)

PCA 4248 | CAS 123875-01-4 is rated 5.0 out of 5 by 1.
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Synonym: Methyl 2-(phenylsulfanyl)ethyl 2,4,6-trimethyl-1,4-dihydropyridine-3,5-dicarboxylate
Application: A competitive inhibitor of PAF at the PAF-R level
CAS Number: 123875-01-4
Purity: 98%
Molecular Weight: 361.4
Molecular Formula: C19H23NO4S
* Refer to Certificate of Analysis for lot specific data (including water content).
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PCA 4248 is a dihydropyridine that has been shown to be a competitive inhibitor of platelet-activating factor (PAF). Mechanistic studies suggest that this compound acts as a competitive antagonist at the PAF-R (PAF receptor) level therefore preventing PAF binding to the receptor. PCA 4248 has also been reported to halt serotonin secretion caused by PAF and also block the increase of eosinophils, neutrophils, and mononuclear cells that result after PAF exposure.


References

1. Martins, M.A., et al. 1993. Eur. J. Pharmacol. 237: 17-22. PMID: 8395390
2. Catalán, R.E., et al. 1995. Eur. J. Pharmacol. 290: 183-188. PMID: 7589212
3. Ranasinghe, S., et al. 2004. Basic Clin. Pharmacol. Toxicol. 95: 87-91. PMID: 15379786

Physical State :
Solid
Solubility :
Soluble in ethanol (100 mM), DMSO (100 mM), and chloroform.
Storage :
Store at -20° C
Melting Point :
165.86° C (Predicted)
Boiling Point :
~497.4° C at 760 mmHg (Predicted)
Density :
~1.2 g/cm3 (Predicted)
Refractive Index :
n20D 1.60
IC50 :
platelet aggregation : IC50 = 1.05 µM (rabbit); [3H]-PAF binding to platelet and PMNL receptors: IC50 = 1 µM (human); PAF-induced platelet aggregation: IC50 = 3.6 µM (human)
Ki Data :
[3H]PAF binding to Platelet activating factor receptor: Ki= 15.09 nM (rabbit)
pK Values :
pKb: 3.32
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
4698
MDL Number :
MFCD00209856
SMILES :
CC1C(=C(NC(=C1C(=O)OCCSC2=CC=CC=C2)C)C)C(=O)OC

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Ranasinghe et al Ranasinghe et al. (PubMed ID 15379786) found that PCA 4248 inhibited the evoked calcium rise in N9 microglial cells. -SCBT Publication Review
Date published: 2015-06-26
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