PAP-1

PAP-1 (5- (4-Phenoxybutoxy) psoralen) is a potent, 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. PAP-1 does not exhibit cytotoxic or phototoxic effects[1][2].

Product Specifications

CAS Number

[870653-45-5]

Product Name Alternative

5- (4-Phenoxybutoxy) psoralen

UNSPSC

12352005

Hazard Statement

H334

Target

Potassium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/PAP-1.html

Purity

99.83

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C1C=CC(C(O1)=CC2=C3C=CO2)=C3OCCCCOC4=CC=CC=C4

Molecular Formula

C21H18O5

Molecular Weight

350.36

Precautions

H334

References & Citations

[1]Schmitz A, et al. Design of PAP-1, a selective small molecule Kv1.3 blocker, for the suppression of effector memory T cells in autoimmune diseases. Mol Pharmacol. 2005 Nov;68 (5) :1254-70.|[2]Pereira LE, et al. Pharmacokinetics, toxicity, and functional studies of the selective Kv1.3 channel blocker 5- (4-phenoxybutoxy) psoralen in rhesus macaques. Exp Biol Med (Maywood) . 2007 Nov;232 (10) :1338-54.