MedChemExpress - Model PAP-1 -870653-45-5
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].MCE products for research use only. We do not sell to patients.
PAP-1
MCE China：PAP-1
Brand：MedChemExpress (MCE)
Cat. No.HY-10015
CAS：870653-45-5
Synonyms：5-(4-Phenoxybutoxy)psoralen
Purity：99.83%
Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Shipping：Room temperature in continental US; may vary elsewhere.
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.
In Vitro：PAP-1 (2-100 nM; 30 minutes) suppresses the proliferation of CCR7-TEM cells with IC50 of 10 nM[1].
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].
IC50 & Target：EC50: 2 nM (Kv1.3), 45 nM (Kv1.5)[1] Cellular Effect Cell Line Type Value Description References
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References：
[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. [Content Brief]
[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. [Content Brief]
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