PPTN hydrochloride 是一种有效，高亲和力，竞争性和高选择性的 P2Y14 受体拮抗剂，K_B 为 434 pM。PPTN hydrochloride 对 P2Y1，P2Y2，P2Y4，P2Y6，P2Y11，P2Y12 或 P2Y13 受体无激动剂或拮抗剂作用。具有抗炎和抗免疫活性。

PPTN hydrochloride is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a K B 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.

Solid

KB: 434 pM (P2Y14 receptor)

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.
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.
PPTN (10 μM) significantly decreases the ratios of p-ERK1/2 to ERK1/2 and p-p38 to p38. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.

In Vitro: DMSO : 250 mg/mL (488.32 mM; Need ultrasonic)配制储备液