Art. -Nr.: HY-10015

PAP-1

(Synonyms: 5-(4-Phenoxybutoxy)psoralen)

13 Cited Publications

Kundenbewertung

Based on 13 publication(s) in Google Scholar

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.

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Reinheit: 99.75%
CAS. Nr.: 870653-45-5
Formel: C₂₁H₁₈O₅
Molecular Weight:350.36

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

PAP-1 Chemical Structure

CAS. Nr.: 870653-45-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

EC50: 2 nM (Kv1.3), 45 nM (Kv1.5)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	3.45 μM Compound: PAP-1	Inhibition of human Kv1.5 ion channel expressed in CHO K1 cells Inhibition of human Kv1.5 ion channel expressed in CHO K1 cells	[PMID: 20974533]
COS-7	IC₅₀	10 μM Compound: PAP-1	Inhibition of human cloned IK1 expressed in african green monkey COS7 cells by whole cell patch clamp assay Inhibition of human cloned IK1 expressed in african green monkey COS7 cells by whole cell patch clamp assay	[PMID: 19282171]
L929	IC₅₀	0.002 μM Compound: 2, PAP-1	Inhibition of Kv1.3 potassium channel expressed in mouse L929 cells by whole cell patch clamp Inhibition of Kv1.3 potassium channel expressed in mouse L929 cells by whole cell patch clamp	[PMID: 19056148]
L929	IC₅₀	2 nM Compound: PAP-1	Inhibition of Kv1.3 expressed in mouse L929 cells exposed to depolarizing step pulses from -80 mV to +40 mV by whole cell patch clamp method Inhibition of Kv1.3 expressed in mouse L929 cells exposed to depolarizing step pulses from -80 mV to +40 mV by whole cell patch clamp method	[PMID: 23084278]
PBMC	EC₅₀	0.4 μM Compound: PAP-1	Immunosuppressant activity in human effector memory T cells of PBMC assessed as inhibition of anti-CD3 antibody-induced cell proliferation by ELISA in presence of 5 uM IK1-blocker 5-(Toluene-4-sulfonyl)-5,6-dihydro-dibenzo[b,d]azepin-7-one Immunosuppressant activity in human effector memory T cells of PBMC assessed as inhibition of anti-CD3 antibody-induced cell proliferation by ELISA in presence of 5 uM IK1-blocker 5-(Toluene-4-sulfonyl)-5,6-dihydro-dibenzo[b,d]azepin-7-one	[PMID: 19282171]
PBMC	EC₅₀	0.43 μM Compound: PAP-1	Immunosuppressant activity in human effector memory T cells of PBMC assessed as inhibition of anti-CD3 antibody-induced cell proliferation by ELISA in presence of 5 uM IK1-blocker TRAM34 Immunosuppressant activity in human effector memory T cells of PBMC assessed as inhibition of anti-CD3 antibody-induced cell proliferation by ELISA in presence of 5 uM IK1-blocker TRAM34	[PMID: 19282171]
PBMC	EC₅₀	0.5 μM Compound: PAP-1	Immunosuppressant activity in human effector memory T cells of PBMC assessed as inhibition of anti-CD3 antibody-induced cell proliferation by ELISA in presence of 16.7 uM IK1-blocker 5-(4-Chloro-benzenesulfonyl)-5,6-dihydro-dibenzo[b,d]azepin-7-one Immunosuppressant activity in human effector memory T cells of PBMC assessed as inhibition of anti-CD3 antibody-induced cell proliferation by ELISA in presence of 16.7 uM IK1-blocker 5-(4-Chloro-benzenesulfonyl)-5,6-dihydro-dibenzo[b,d]azepin-7-one	[PMID: 19282171]
PBMC	EC₅₀	1.2 μM Compound: PAP-1	Immunosuppressant activity in human effector memory T cells of PBMC assessed as inhibition of anti-CD3 antibody-induced cell proliferation by ELISA in presence of 5 uM IK1-blocker 5-(4-Chloro-benzenesulfonyl)-5,6-dihydro-dibenzo[b,d]azepin-7-one Immunosuppressant activity in human effector memory T cells of PBMC assessed as inhibition of anti-CD3 antibody-induced cell proliferation by ELISA in presence of 5 uM IK1-blocker 5-(4-Chloro-benzenesulfonyl)-5,6-dihydro-dibenzo[b,d]azepin-7-one	[PMID: 19282171]
PBMC	EC₅₀	25 μM Compound: PAP-1	Immunosuppressant activity in human effector memory T cells of PBMC assessed as inhibition of anti-CD3 antibody-induced cell proliferation by ELISA Immunosuppressant activity in human effector memory T cells of PBMC assessed as inhibition of anti-CD3 antibody-induced cell proliferation by ELISA	[PMID: 19282171]

In Vitro

PAP-1 (2-100 nM; 30 minutes) suppresses the proliferation of CCR7-TEM cells with IC₅₀ of 10 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

CCR7-TEM cells (anti-CD3 Ab stimulated)
Concentration:

2, 10, 25, 100 nM
Incubation Time:

30 minutes
Result:

Suppresses the Proliferation of CCR7-TEM cells with IC50 of 10 nM.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

9- to 11- week-old female Lewis rats^[1]
Dosage:

Intraperitoneal injection; three times daily for 48 hours
Administration:

0.3, 1, 3 mg/kg
Result:

Dose-dependently suppressed the DTH reaction.

Chemical Information

CAS. Nr. 870653-45-5
Appearance Solid
Molecular Weight 350.36
Formel C₂₁H₁₈O₅
Color White to yellow
SMILES

O=C1C=CC(C(O1)=CC2=C3C=CO2)=C3OCCCCOC4=CC=CC=C4
Synonyms

5-(4-Phenoxybutoxy)psoralen
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (13)

All Cell Proliferation/Viability AssayIFIn Vivo Efficacy StudyHistological Imaging/Staining

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Journal Impact Factor

Cell Res

The axon initial segment-associated microglia regulate neuronal activity and visual perception. [Abstract]

2026 Jan 28. PMID: 41593328
Cell Mol Immunol

NLRP3-dependent pyroptosis is required for HIV-1 gp120-induced neuropathology. [Abstract]

2020 Mar;17(3):283-299. PMID: 31320730
Nat Commun

Kir2.1-mediated membrane potential promotes nutrient acquisition and inflammation through regulation of nutrient transporters. [Abstract]

2022 Jun 21;13(1):3544. PMID: 35729093
Drug Deliv

Reliable high-PAP-1-loaded polymeric micelles for cancer therapy: preparation, characterization, and evaluation of anti-tumor efficacy. [Abstract]

2025 Dec;32(1):2490269. PMID: 40207975

PAP-1 purchased from MedChemExpress. Usage Cited in: Drug Deliv. 2025 Dec;32(1):2490269. [Abstract]

Effects of PAP-1 (1-50 μM; 24 h) and different PAP-1 formulations on the viability of Jurkat and B16F10 cells. PAP-1-loaded polymeric micelles reduced cell viability more strongly than free PAP-1.

PAP-1 purchased from MedChemExpress. Usage Cited in: Drug Deliv. 2025 Dec;32(1):2490269. [Abstract]

CLSM images of immunofluorescence, depicting caspase-3 activity and the effect apoptosis on jurkat cells exposed to various PAP-1 formulations at a concentration of 50 μmol/L for 24 hours. PAP-1 and PAP-1 combined with MDRi slightly increased caspase-3 activity, whereas cells treated with PAP-1-loaded PMs showed significant enhancement in caspase-3 activity.

PAP-1 purchased from MedChemExpress. Usage Cited in: Drug Deliv. 2025 Dec;32(1):2490269. [Abstract]

Antitumor effects of diverse PAP-1 formulations (7 or 14 μg/g; i.p.; administered on days 5, 7, 9, and 11 after tumor inoculation) in B16F10 melanoma mouse model. PAP-1 PMs treatment exhibited remarkable tumor suppression, reducing tumor volume by 88.23% and 94.26% in the low and high-dose groups, respectively.

PAP-1 purchased from MedChemExpress. Usage Cited in: Drug Deliv. 2025 Dec;32(1):2490269. [Abstract]

Hematoxylin/eosin staining from the heart, liver, spleen, lung, kidney, small intestine, and brain in the groups treated by different PAP-1 formulations (7 or 14 μg/g; i.p.; administered on days 5, 7, 9, and 11 after tumor inoculation). No discernible histological damage was observed in the examined major organs.
J Ethnopharmacol

BmKK2, a thermostable Kv1.3 blocker from Buthus martensii Karsch (BmK) scorpion, inhibits the activation of macrophages via Kv1.3-NF-κB- NLPR3 axis. [Abstract]

2023 Oct 5:314:116624. PMID: 37182676

PAP-1 purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2023 Oct 5:314:116624. [Abstract]

Serum TNF-α and IL-1β concentrations in C57BL/6 mice at 2 h after intraperitoneal administration of LPS and PAP-1 (5 mg/kg; single dose; 24 h). PAP-1 significantly inhibited the LPS-induced increases in serum TNF-α and IL-1β levels.
Neurobiol Dis

Microglial TREM2 deficiency causes E/I imbalance and triggers ASD-like behaviors by altering potassium channel Kv1.3 activation. [Abstract]

2025 Dec:217:107185. PMID: 41213335
Int J Mol Sci

Bergamottin and PAP-1 Induced ACE2 Degradation to Alleviate Infection of SARS-CoV-2. [Abstract]

2022 Oct 19;23(20):12565. PMID: 36293419
Sci Rep

Activation/inactivation of Tregs mediated by Kv1.3 potassium channels synergistically with exosome secretion to regulate myocardial fibrosis. [Abstract]

2025 Dec 1;15(1):45756. PMID: 41326524
Exp Neurol

Kv1.3 channel blockade alleviates cerebral ischemia/reperfusion injury by reshaping M1/M2 phenotypes and compromising the activation of NLRP3 inflammasome in microglia. [Abstract]

2020 Oct;332:113399. PMID: 32652099
Brain Res Bull

Pharmacological inhibition of Kv1.3 channel reduces sevoflurane-induced cognitive impairment through NLRP3-dependent microglial modulation. [Abstract]

2025 Apr 17:111351. PMID: 40252702
FASEB J

The Kv1.3 ion channel acts as a host factor restricting viral entry. [Abstract]

2021 Feb;35(2):e20995. PMID: 32910509
J Integr Neurosci

Kv1.3 Blockade Alleviates White Matter Injury through Reshaping M1/M2 Phenotypes via the NF-κB Signaling Pathway after Intracerebral Hemorrhage. [Abstract]

2023 Dec 5;22(6):171. PMID: 38176920
Research Square Print

November 28th, 2022.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (142.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8542 mL

14.2710 mL

28.5421 mL

5 mM

0.5708 mL

2.8542 mL

5.7084 mL

10 mM

0.2854 mL

1.4271 mL

2.8542 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.14 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (7.14 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.14 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8542 mL	14.2710 mL	28.5421 mL	71.3552 mL
	5 mM	0.5708 mL	2.8542 mL	5.7084 mL	14.2710 mL
	10 mM	0.2854 mL	1.4271 mL	2.8542 mL	7.1355 mL
	15 mM	0.1903 mL	0.9514 mL	1.9028 mL	4.7570 mL
	20 mM	0.1427 mL	0.7136 mL	1.4271 mL	3.5678 mL
	25 mM	0.1142 mL	0.5708 mL	1.1417 mL	2.8542 mL
	30 mM	0.0951 mL	0.4757 mL	0.9514 mL	2.3785 mL
	40 mM	0.0714 mL	0.3568 mL	0.7136 mL	1.7839 mL
	50 mM	0.0571 mL	0.2854 mL	0.5708 mL	1.4271 mL
	60 mM	0.0476 mL	0.2379 mL	0.4757 mL	1.1893 mL
	80 mM	0.0357 mL	0.1784 mL	0.3568 mL	0.8919 mL
	100 mM	0.0285 mL	0.1427 mL	0.2854 mL	0.7136 mL

Keywords

PAP-1

13 Cited Publications

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PAP-1

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Targeted Diversity Library

Potassium Channel Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) PAP-1

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PAP-1

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Targeted Diversity Library

Potassium Channel Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) PAP-1

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PAP-1 Related Classifications

HY-10015 Related Classifications