PAP-1 是口服活性的Kv1.3选择性阻滞剂 (EC50=2 nM)。它依赖性阻止 Kv1.3，并优先与通道的 C 型失活状态结合来发挥作用。

PAP-1 is a selective, and orally active Kv1.3 blocker (EC50: 2 nM).

PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50: 45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels [1, 2]. PAP-1 (2-100 nM; 30 minutes) suppresses the proliferation of CCR7-TEM cells (IC50: 10 nM) [1].

PAP-1 (0.3-3 mg/kg; i.p.; three times daily for 48 hours) prevents delayed type hypersensitivity (DTH) in lewis rats [1].

Cell Line: CCR7-TEM cells (anti-CD3 Ab stimulated). Concentration: 2, 10, 25, 100 nM. Incubation Time: 30 minutes [1]

Animal Model: 9- to 11- week-old female Lewis rats. Dosage: I.P.; three times daily for 48 hours. Administration: 0.3, 1, 3 mg/kg [1]

870653-45-5

C21H18O5

350.36

5-(4-Phenoxybutoxy)psoralen

DMSO:48 mg/mL (137 mM),Need ultrasonic
H2O:Insoluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years