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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.
| Molecular Weight | 350.36 |
| CAS Number | 870653-45-5 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Kam Leung. 99m Tc-Mercaptoacetyl-Gly-Gly-Gly-PAP-1
[5] H Maita, et al. PAP-1, a novel target protein of phosphorylation by pim-1 kinase
| Related Potassium Channel Products |
|---|
| TAK-438
TAK-438 is a novel and potent potassium-competitive acid blocker (P-CAB) with IC50 of 19 nM. |
| ML133 hydrochloride
ML133 hydrochloride is a selective inhibitor of the Kir2 family of inward rectifier (IRK, KCNJ) potassium channels. |
| Doxapram hydrochloride hydrate
Doxapram hydrochloride hydrate inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively. |
| Gliquidone
Gliquidone is an ATP-sensitive K+ channel antagonist with IC50 of 27.2 nM. |
| Pinacidil monohydrate
Pinacidil monohydrate is known to augment a time-independent outward current in cardiac tissues by activating the ATP-regulated potassium channels. |
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