PAP-1

• UNSPSC Description:

  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].

• Target Antigen:

  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 Weight:

  350.36

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  No Development Reported

• CAS Number:

  870653-45-5