| Bioactivity | PPTN is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. PPTN exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and immune activity[1]. |
| Target | KB: 434 pM (P2Y14 receptor) |
| Invitro | 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]. |
| Name | PPTN |
| CAS | 1160271-30-6 |
| Formula | C29H24F3NO2 |
| Molar Mass | 475.50 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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. |