5-(4-苯氧基丁氧基)补骨脂素(PAP-1)

• 常用名: 5-(4-苯氧基丁氧基)补骨脂素(PAP-1)
• 英文名: PAP-1
• CAS号: 870653-45-5
• 分子量: 350.365
• 密度: 1.3±0.1 g/cm3
• 沸点: 555.8±50.0 °C at 760 mmHg
• 分子式: C₂₁H₁₈O₅
• 熔点: N/A
• 闪点: 289.9±30.1 °C

5-(4-苯氧基丁氧基)补骨脂素(PAP-1)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].

5-(4-苯氧基丁氧基)补骨脂素(PAP-1)名称

• 中文名: 4-(4-苯氧基丁氧基)-7H-呋喃并[3,2-G][1]苯并吡喃-7-酮
• 英文名: 5-(4-Phenoxybutoxy)psoralen
• 中文别名: 5-(4-苯氧基丁氧基) | Kv1.3抑制剂 | 5-(4-苯氧基丁氧基)补骨脂素 | 4-(4-苯氧基丁氧基)-7H-呋喃并(3,2-g)(1)苯并吡喃-7-酮

5-(4-苯氧基丁氧基)补骨脂素(PAP-1)物理化学性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 555.8±50.0 °C at 760 mmHg
• 分子式: C₂₁H₁₈O₅
• 分子量: 350.365
• 闪点: 289.9±30.1 °C
• 精确质量: 350.115417
• PSA: 61.81000
• LogP: 4.56
• 蒸汽压: 0.0±1.5 mmHg at 25°C
• 折射率: 1.619
• 储存条件: 2~8°C

5-(4-苯氧基丁氧基)补骨脂素(PAP-1)安全信息

• 风险声明 (欧洲): R42/43
• 安全声明 (欧洲): 22-36/37-45
• 海关编码: 2932999099

5-(4-苯氧基丁氧基)补骨脂素(PAP-1)英文别名

• 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