| Bioactivity | 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 | EC50: 2 nM (Kv1.3), 45 nM (Kv1.5) | ||||||||||||
| Invitro | PAP-1 (2-100 nM; 30 minutes) suppresses the proliferation of CCR7-TEM cells with IC50 of 10 nM[1]. Cell Proliferation Assay[1] Cell Line: | ||||||||||||
| In Vivo | PAP-1 (0.3-3 mg/kg; i.p.; three times daily for 48 hours) prevents delayed type hypersensitivity (DTH) in lewis rats[1]. Animal Model: | ||||||||||||
| Name | PAP-1 | ||||||||||||
| CAS | 870653-45-5 | ||||||||||||
| Formula | C21H18O5 | ||||||||||||
| Molar Mass | 350.36 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |