For research use only. Not for therapeutic Use.
PPTN hydrochloride is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. PPTN hydrochloride exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and anti-immune activity[1].
PPTN exhibits strong selectivity for the P2Y14-R over the other seven nucleotide-activated P2Y receptors. 1 μM PPTN exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors[1].
PPTN inhibits UDP-glucose-promoted chemotaxis in differentiated HL-60 human promyelocytic leukemia cells with IC50s of ~1 nM in the presence of 10 μM UDP-glucose and ~4 nM in the presence of 100 μM[1].
PPTN (10 µM) significantly decreases the ratios of p-ERK1/2 to ERK1/2 and p-p38 to p38[2].
| Catalog Number | I045633 |
| CAS Number | 1992047-65-0 |
| Synonyms | 4-(4-piperidin-4-ylphenyl)-7-[4-(trifluoromethyl)phenyl]naphthalene-2-carboxylic acid;hydrochloride |
| Molecular Formula | C29H25ClF3NO2 |
| Purity | ≥95% |
| InChI | InChI=1S/C29H24F3NO2.ClH/c30-29(31,32)25-8-5-19(6-9-25)22-7-10-26-23(15-22)16-24(28(34)35)17-27(26)21-3-1-18(2-4-21)20-11-13-33-14-12-20;/h1-10,15-17,20,33H,11-14H2,(H,34,35);1H |
| InChIKey | FKMVYPCBLWYNAV-UHFFFAOYSA-N |
| SMILES | C1CNCCC1C2=CC=C(C=C2)C3=C4C=CC(=CC4=CC(=C3)C(=O)O)C5=CC=C(C=C5)C(F)(F)F.Cl |
| Reference | [1]. Barrett MO, et al. A selective high-affinity antagonist of the P2Y14 receptor inhibits UDP-glucose-stimulated chemotaxis of human neutrophils. Mol Pharmacol. 2013 Jul;84(1):41-9. [2]. Lin J, et al. The P2Y14 receptor in the trigeminal ganglion contributes to the maintenance of inflammatory pain. Neurochem Int. 2019 Dec;131:104567. |
