PAP-1

SKU: orb1296152

Description

PAP-1 is a potent and selective small molecule inhibitor of the Kv1.3 potassium channel, exhibiting an EC50 of 2 nM and oral bioavailability. Its research applications include in vitro electrophysiology studies and in vivo models for investigating T cell-mediated autoimmune diseases, such as multiple sclerosis and type-1 diabetes.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 870653-45-5
• MW: 350.36
• Purity: 99.75% (May vary between batches)
• Formula: C₂₁H₁₈O₅
• SMILES: O=c1ccc2c(OCCCCOc3ccccc3)c3ccoc3cc2o1
• Target: Potassium Channel
• Solubility: DMSO:50 mg/mL (142.71 mM);H2O:Insoluble;10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.71 mM)

Bioactivity

• Target IC50:
  Kv1.5 channel:45 nM (EC50)|Kv1.3 channel:2 nM (EC50)
• In Vivo:
  PAP-1 (0.3-3 mg/kg; i.p.; thrice daily for 48 hours) prevents delayed type hypersensitivity (DTH) in Lewis rats .
• In Vitro:
  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) .
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• Cell Research:
  Cell Line: CCR7-TEM cells (anti-CD3 Ab stimulated). Concentration: 2, 10, 25, 100 nM. Incubation Time: 30 minutes
• Animal Research:
  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

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

5-(4-Phenoxybutoxy)psoralen, Inhibitor, PAP 1, PAP-1, PAP1, KcsA, Kv1.3 channels, inhibit, Potassium Channel, PotassiumChannel

Compound Identifiers

PubChem CID

11302540