| Name | PAP-1 |
| Description | PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a selective, orally active Kv1.3 blocker with an EC50 of 2 nM. |
| Cell Research | Cell Line: CCR7-TEM cells (anti-CD3 Ab stimulated). Concentration: 2, 10, 25, 100 nM. Incubation Time: 30 minutes [1] |
| 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 [1] |
| 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) [1]. |
| In vivo | PAP-1 (0.3-3 mg/kg; i.p.; thrice daily for 48 hours) prevents delayed type hypersensitivity (DTH) in Lewis rats [1]. |
| Storage | 02 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (142.71 mM), Sonication is recommended. H2O : Insoluble 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.71 mM), Sonication is recommended.
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| Keywords | PotassiumChannel | Potassium Channel | PAP-1 | PAP1 | PAP 1 | Kv1.3 channels | KcsA | Inhibitor | inhibit |
| Inhibitors Related | Minoxidil sulfate | Tannic acid | Hydrochlorothiazide | 1,8-Cineole | Tetraethylammonium bromide | Ursodeoxycholic acid | Chenodeoxycholic acid | Minoxidil | Chlorzoxazone | 2,2,2-Trichloroethanol | Taurocholic acid sodium salt hydrate | Indapamide |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Orally Active Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Potassium Channel Targeted Library | Ion Channel Targeted Library | Anti-Cancer Drug Library |