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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 20 mg/mL (57.08 mM), Sonication is recommended. H2O : Insoluble
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Keywords | PAP-1 | KcsA | Potassium Channel | inhibit | PAP1 | Inhibitor | PAP 1 |
Inhibitors Related | Minoxidil sulfate | Quinine | (±)-Naringenin | Tolbutamide | Tetraethylammonium bromide | Halothane | Butamben | Tetraethylammonium chloride | Cloperastine hydrochloride | 2,2,2-Trichloroethanol | Chlorzoxazone | Indapamide |
Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Potassium Channel Targeted Library | Ion Channel Targeted Library | Anti-Cancer Drug Library |