PAP-1

Modify Date: 2025-08-21 16:23:35

PAP-1 Structure
PAP-1 structure
 Common Name PAP-1
CAS Number 870653-45-5 Molecular Weight 350.365
Density 1.3±0.1 g/cm3 Boiling Point 555.8±50.0 °C at 760 mmHg
Molecular Formula C21H18O5 Melting Point N/A
MSDS USA Flash Point 289.9±30.1 °C
Symbol GHS08
GHS08		 Signal Word Danger

 Use of PAP-1


PAP-1 is a selective inhibitor of Kv1.3, voltage-gated K+ channel. PAP-1 (EC50=2 nM) potently inhibits human T effector memory cell proliferation and delayed hypersensitivity. IC50 value: 2 nM (EC50) [1]in vitro: blocks Kv1.3 in a use-dependent manner, with a Hill coefficient of 2 and an EC50 of 2 nM, by preferentially binding to the C-type inactivated state of the channel. PAP-1 is 23-fold selective over Kv1.5, 33- to 125-fold selective over other Kv1-family channels, and 500- to 7500-fold selective over Kv2.1, Kv3.1, Kv3.2, Kv4.2, HERG, calcium-activated K+ channels, Na+,Ca2+, and Cl- channels [1]. The blockade of Kv1.3 results in membrane depolarization and inhibition of TEM proliferation and function. In this study, the in vitro effects of PAP-1 on T cells and the in vivo toxicity and pharmacokinetics (PK) were examined in rhesus macaques (RM) with the ultimate aim of utilizing PAP-1 to define the role of TEMs in RM infected with simian immunodeficiency virus (SIV). Electrophysiologic studies on T cells in RM revealed a Kv1.3 expression pattern similar to that in human T cells. Thus, PAP-1 effectively suppressed TEM proliferation in RM [2].in vivo: PAP-1 does not exhibit cytotoxic or phototoxic effects, is negative in the Ames test, and affects cytochrome P450-dependent enzymes only at micromolar concentrations. PAP-1 potently inhibits the proliferation of human TEM cells and suppresses delayed type hypersensitivity, a TEM cell-mediated reaction, in rats [1]. When administered intravenously, PAP-1 showed a half-life of 6.4 hrs; the volume of distribution suggested extensive distribution into extravascular compartments. When orally administered, PAP-1 was efficiently absorbed. Plasma concentrations in RM undergoing a 30-day, chronic dosing study indicated that PAP-1 levels suppressive to TEMs in vitro can be achieved and maintained in vivo at a non-toxic dose [2].

 Names

Name 5-(4-Phenoxybutoxy)psoralen
Synonym More Synonyms

 PAP-1 Biological Activity

Description PAP-1 is a selective inhibitor of Kv1.3, voltage-gated K+ channel. PAP-1 (EC50=2 nM) potently inhibits human T effector memory cell proliferation and delayed hypersensitivity. IC50 value: 2 nM (EC50) [1]in vitro: blocks Kv1.3 in a use-dependent manner, with a Hill coefficient of 2 and an EC50 of 2 nM, by preferentially binding to the C-type inactivated state of the channel. PAP-1 is 23-fold selective over Kv1.5, 33- to 125-fold selective over other Kv1-family channels, and 500- to 7500-fold selective over Kv2.1, Kv3.1, Kv3.2, Kv4.2, HERG, calcium-activated K+ channels, Na+,Ca2+, and Cl- channels [1]. The blockade of Kv1.3 results in membrane depolarization and inhibition of TEM proliferation and function. In this study, the in vitro effects of PAP-1 on T cells and the in vivo toxicity and pharmacokinetics (PK) were examined in rhesus macaques (RM) with the ultimate aim of utilizing PAP-1 to define the role of TEMs in RM infected with simian immunodeficiency virus (SIV). Electrophysiologic studies on T cells in RM revealed a Kv1.3 expression pattern similar to that in human T cells. Thus, PAP-1 effectively suppressed TEM proliferation in RM [2].in vivo: PAP-1 does not exhibit cytotoxic or phototoxic effects, is negative in the Ames test, and affects cytochrome P450-dependent enzymes only at micromolar concentrations. PAP-1 potently inhibits the proliferation of human TEM cells and suppresses delayed type hypersensitivity, a TEM cell-mediated reaction, in rats [1]. When administered intravenously, PAP-1 showed a half-life of 6.4 hrs; the volume of distribution suggested extensive distribution into extravascular compartments. When orally administered, PAP-1 was efficiently absorbed. Plasma concentrations in RM undergoing a 30-day, chronic dosing study indicated that PAP-1 levels suppressive to TEMs in vitro can be achieved and maintained in vivo at a non-toxic dose [2].
Related Catalog
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.

[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.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 555.8±50.0 °C at 760 mmHg
Molecular Formula C21H18O5
Molecular Weight 350.365
Flash Point 289.9±30.1 °C
Exact Mass 350.115417
PSA 61.81000
LogP 4.56
Vapour Pressure 0.0±1.5 mmHg at 25°C
Index of Refraction 1.619
Storage condition 2~8°C

 Safety Information

Symbol GHS08
GHS08
Signal Word Danger
Hazard Statements H334
Precautionary Statements P261-P342 + P311
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Faceshields;Gloves
Risk Phrases R42/43
Safety Phrases 22-36/37-45
RIDADR NONH for all modes of transport
HS Code 2932999099

 Customs

HS Code 2932999099
Summary 2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

7H-Furo[3,2-g][1]benzopyran-7-one, 4-(4-phenoxybutoxy)-
4-(4-phenoxybutoxy)furo[3,2-g]chromen-7-one
4-(4-Phenoxybutoxy)-7H-furo[3,2-g]chromen-7-one
5-(4-Phenoxybutoxy)psoralen
PAP-1
The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.
Top Suppliers:I want be here

Get all suppliers and price by the below link:

PAP-1 suppliers

Price: ￥600.6/5mg

Reference only. check more PAP-1 price

Related Compounds: More...
pap
3973-17-9
3-anilinopropane-1,2-diol
5840-15-3
2-amino-6-imino-5-(2-phenylhydrazinyl)pyridin-3-one
86271-56-9
Propane,1,1-bis(ethylsulfonyl)-2-methyl-
6330-46-7
Pyridinium, 1- (2-hydroxy[1,1:3,1-terphenyl]-5-yl)-2,4, 6-triphenyl-, perchlorate (salt)
14514-74-0
Cyclohexanecarboxylicacid, 1-methyl-3-oxo-, ethyl ester
7356-04-9
2-[1-(2-hydroxy-3,5-dimethylphenyl)cyclohexyl]-4,6-dimethylphenol
144146-25-8
3-[1-(2,5-dimethylthiophen-3-yl)octadecyl]-4-propan-2-ylideneoxolane-2,5-dione
144137-47-3
trans-1,2-Dimethylcyclohexane
6876-23-9
N-((6-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)-3-(2-methoxyphenyl)propanamide
2034354-63-5
N-((6-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)-2-(methylthio)nicotinamide
2034416-50-5
6-(cyclopentyloxy)-N-((6-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)nicotinamide
2034371-84-9
2-(2-fluorophenoxy)-N-((6-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)propanamide
2034550-42-8
N-((6-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)-3-(methylthio)benzamide
2034371-90-7
(E)-N-((6-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)-2-methyl-3-phenylacrylamide
2035008-37-6
2-(2-chloro-6-fluorophenyl)-N-((6-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)acetamide
2034371-96-3
3-(1H-benzo[d]imidazol-2-yl)-N-((6-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)propanamide
2034550-50-8
N-((6-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)-1-methyl-1H-pyrazole-5-carboxamide
2034326-35-5
1-ethyl-N-((6-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)-1H-pyrazole-3-carboxamide
2034416-68-5
Chemsrc provides PAP-1(CAS#:870653-45-5) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of PAP-1 are included as well.>> amp version: PAP-1

Home | MSDS/SDS Database Search | Journals | Product Classification | Biologically Active Compounds | Selling Leads | About Us | Disclaimer

Copyright © 2024 ChemSrc All Rights Reserved