CAS:870653-45-5PAP-1

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PAP-1 4-(4-苯氧基丁氧基)-7H-呋喃并[3,2-G][1]苯并吡喃-7-酮 Cat No. FB02585Cas No. 870653-45-5

Synonyms: 5-(4-Phenoxybutoxy)psoralen

PAP-1 is a selective inhibitor of Kv1.3, voltage-gated K+ channel, it potently inhibits human T effector memory cell proliferation with EC50 of 2 nM and delayed hypersensitivity.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8541 mL
- 14.2706 mL
- 28.5413 mL
- 5 mM
- 0.5708 mL
- 2.8541 mL
- 5.7083 mL
- 10 mM
- 0.2854 mL
- 1.4271 mL
- 2.8541 mL
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技术信息

CAS号

870653-45-5

储存条件

粉末: -20°C 3 年

液体: -80°C 12 月

分子式

C21H18O5

运输

蓝冰

分子量

350.37

别名

5-(4-Phenoxybutoxy)psoralen

溶解度

DMSO	50.0 mg/mL (142.7 mM) warming
Water	Insoluble

动物实验配方

靶点数据

生物活性

靶点 Potassium Channel KV1.3

EC50:2nM
描述PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50 = 2 nM). 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. 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 (memory T cells) cell-mediated reaction, in rats^[3]. PAP-1 effectively suppressed TEM proliferation in RM (rhesus macaques). 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. PAP-1 selectively inhibited the TEM function in vivo, as indicated by a modest reactivation of cytomegalovirus (CMV) replication^[4].