5-(4-苯氧基丁氧基)补骨脂素(PAP-1)

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发布时间： 2024-07-15 12:37:12

CAS号：870653-45-5

常用名： 5-(4-苯氧基丁氧基)补骨脂素(PAP-1)

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纯度： 98.0%

备货期： 10天

库存： 现货

其他详情（用途，包装）：
用途： 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]. 物理化学性质： CAS号：870653-45-5 常用中文名：5-(4-苯氧基丁氧基)补骨脂素(PAP-1) 常用英文名：PAP-1 分子式：C21H18O5 分子量：350.365 密度：1.3±0.1 g/cm3 沸点：555.8±50.0 °C at 760 mmHg 熔点：N/A 闪点：289.9±30.1 °C 储存条件：2~8°C

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2022-03-04 价格：￥241.9 5-(4-苯氧基丁氧基)补骨脂素（PAP-1）

2024-07-15 价格：需询单 5-(4-苯氧基丁氧基)补骨脂素(PAP-1)

2019-03-05 价格：￥428.0 5-(4-苯氧基丁氧基)补骨脂素(PAP-1)

2022-05-12 价格：$需询单 PAP-1,5-(4-Phenoxybutoxy)psoralen

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5-(4-苯氧基丁氧基)补骨脂素(PAP-1)价格

5-(4-苯氧基丁氧基)补骨脂素(PAP-1)

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