5-(4-苯氧基丁氧基)补骨脂素(PAP-1)
更新时间：2025-08-27 09:50:02
采购访问：36次
| 常用名 | 5-(4-苯氧基丁氧基)补骨脂素(PAP-1) | CAS号 | 870653-45-5 |
|---|---|---|---|
| 价格 | 纯度 | 98.0% | |
| 备货期 | 10天 | 库存 | 现货 |
| 产品详情（用途，包装等）
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 |
上海化源世纪贸易有限公司
认证状态：已认证供应商
商品数：396716件
电话：53555033
地址：上海市普陀区金沙江路1759号圣诺亚大厦B座
地区： 上海市 上海市 普陀区
联系人：徐经理
联系人电话：133 1186 9306
邮件：xuqm@chemsrc.com
网址：http://www.chemsrc.com
主要市场：
年贸易额：
外贸占销售比例：
主要合作伙伴：
- 上海化源世纪贸易有限公司
- 上海市 上海市 普陀区
- 产品名：5-(4-苯氧基丁氧基)补骨脂素(PAP-1)
- 价格：
- 纯度：98.0%
- 备货期：10天
- 联系人：徐经理
查看所有供应商和价格请点击：
参考价格：￥600.6/5mg