|4-(4-苯氧基丁氧基)-7H-呋喃并[3,2-G][1]苯并吡喃-7-酮|CsnPharm

CAS No.: 870653-45-5

PAP-1/5-(4-苯氧基丁氧基)补骨脂素（PAP-1） Catalog No. CSN10033

Synonyms: 5-(4-Phenoxybutoxy)psoralen;SPS-4251;AS-77

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.

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靶点选择性

生物活性

实验方案

技术信息

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].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01349920	-	-	Completed	-	-
NCT00564109	-	-	Unknown	-	Switzerland ... more >> Recruiting Zurich, Switzerland Collapse <<
NCT01258179	-	-	Terminated(low recruitment)	-	Switzerland ... more >> Department of Visceral and Transplantation Surgery Zurich, CH/Zürich, Switzerland, 8091 Collapse <<

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参考文献

[1] Pereira LE, Villinger F, 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.
[2] 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.
[3] Schmitz A, Sankaranarayanan A, Azam P, 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;68(5):1254-1270
[4] Pereira LE, Villinger F, Wulff H, Sankaranarayanan A, Raman G, Ansari AA. Pharmacokinetics, toxicity, and functional studies of the selective Kv1.3 channel blocker 5-(4-phenoxybutoxy)psoralen in rhesus macaques. Exp Biol Med (Maywood). 2007;232(10):1338-1354

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8542 mL
- 14.2708 mL
- 28.5417 mL
- 5 mM
- 0.5708 mL
- 2.8542 mL
- 5.7083 mL
- 10 mM
- 0.2854 mL
- 1.4271 mL
- 2.8542 mL

技术信息

CAS号

870653-45-5

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H18O5

运输

蓝冰

分子量

350.36

别名

5-(4-Phenoxybutoxy)psoralen;SPS-4251;AS-77

溶解度

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

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PAP-1/5-(4-苯氧基丁氧基)补骨脂素（PAP-1） Catalog No. CSN10033

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