PAP-1

Catalog No.E0378 Batch:E037801

Technical Data

Formula	C₂₁H₁₈O₅
Molecular Weight	350.37	CAS No.	870653-45-5
Solubility (25°C)*	In vitro	DMSO	70 mg/mL (199.78 mM)
		Ethanol	25 mg/mL (71.35 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

PAP-1 (5-(4-phenoxybutoxy)psoralen), a Kv1.3 antagonist with an EC50 of 2 nM, inhibits the proliferation of human T cells and suppresses delayed type hypersensitivity in rats.

Targets

Kv1.3 ^[1]

2 nM(EC50)

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]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines CCR7-TEM cells Concentrations 2-100 nM Incubation Time 30 min Method CCR7- T cells are then seeded at 5 X 104 per well together with 5 X 104 autologous irradiated peripheral blood mononuclear cells in RPMI culture medium into round-bottomed, 96-well plates. PAP-1 is added at different concentrations, and the cells are stimulated with 25 ng/ml soluble anti-CD3 Ab 30 min later. Cells are harvested onto glassfiber filters, and radioactivity is measured in a ß-scintillation counter.

Cell Assay:^{^[1]}

Cell lines
CCR7-TEM cells
Concentrations
2-100 nM
Incubation Time
30 min
Method
CCR7- T cells are then seeded at 5 X 104 per well together with 5 X 104 autologous irradiated peripheral blood mononuclear cells in RPMI culture medium into round-bottomed, 96-well plates. PAP-1 is added at different concentrations, and the cells are stimulated with 25 ng/ml soluble anti-CD3 Ab 30 min later. Cells are harvested onto glassfiber filters, and radioactivity is measured in a ß-scintillation counter.

References

[1] Schmitz A, et al. Mol Pharmacol. 2005 Nov;68(5):1254-70.

Selleck's PAP-1 has been cited by 2 publications

Immunosuppressive effects of new thiophene-based KV1.3 inhibitors [ Eur J Med Chem, 2023, 259:115561]	PubMed: 37454520
Bergapten attenuates microglia-mediated neuroinflammation and ischemic brain injury by targeting Kv1.3 and Carbonyl reductase 1 [ Eur J Pharmacol, 2022, 933:175242]	PubMed: 36058290

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SHIPPING AND STORAGE
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