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Membrane transporter/Ion channel Potassium Channel PAP-1

PAP-1

Catalog No. TQ0179   CAS 870653-45-5
Synonyms: 5-(4-Phenoxybutoxy)psoralen

PAP-1 is a selective, and orally active Kv1.3 blocker (EC50: 2 nM).

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PAP-1, CAS 870653-45-5
Pack Size Availability Price/USD Quantity
2 mg In stock 57.00
5 mg In stock 81.00
10 mg In stock 138.00
25 mg In stock 307.00
50 mg In stock 547.00
100 mg In stock 918.00
200 mg In stock 1378.00
1 mL * 10 mM (in DMSO) In stock 92.00
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Purity 99.49%
Biological Description
Chemical Properties
Storage & Solubility Information
Description PAP-1 is a selective, and orally active Kv1.3 blocker (EC50: 2 nM).
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.; three times daily for 48 hours) prevents delayed type hypersensitivity (DTH) in lewis rats [1].
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]
Synonyms 5-(4-Phenoxybutoxy)psoralen
Purity 99.49%
Molecular Weight 350.36
Formula C21H18O5
CAS No. 870653-45-5

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 6 months

Solubility Information

DMSO: 48 mg/mL (137 mM), Need ultrasonic

Water: Insoluble

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
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.

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