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质量水平
检测方案
≥98% (HPLC)
形式
solid
储存条件
protect from light
颜色
white
溶解性
DMSO: 9 mg/mL
储存温度
2-8°C
SMILES字符串
O=C1Oc2cc3occc3c(OCCCCOc4ccccc4)c2C=C1
InChI
1S/C21H18O5/c22-20-9-8-16-19(26-20)14-18-17(10-13-24-18)21(16)25-12-5-4-11-23-15-6-2-1-3-7-15/h1-3,6-10,13-14H,4-5,11-12H2
InChI key
KINMYBBFQRSVLL-UHFFFAOYSA-N
生化/生理作用
5-（4-苯氧基丁氧基）补骨脂素（PAP-1） 源自天然化合物 5-甲氧基补骨脂素。PAP-1 对 Kv1.3（电压门控钾通道）的选择性高于其他 Kv1 家族成员。Kv1.3 主要存在于激活的效应记忆 T 细胞的细胞膜上。Kv1.3 的抑制导致膜去极化。在大鼠模型中，已知 PAP-1 可以延缓糖尿病的发作。它可能用于治疗银屑病和效应记忆 T 细胞介导的自身免疫性疾病。PAP-1 的口服、腹膜内和局部给药可预防恶唑酮诱导的过敏性接触性皮炎。
Kv1.3 的选择性抑制剂，电压门控 K+ 通道。PAP-1（EC50=2 nM） 有效抑制人 T 效应记忆细胞增殖和延迟超敏反应。口服或腹腔内有效。5-（4-苯氧基丁氧基）补骨脂素对 Kv1.3 的选择性比 Kv1.5 高 23 倍，比其他 Kv1 家族通道的选择性高 33-125 倍。
警示用语：
Danger
危险声明
预防措施声明
危险分类
Resp. Sens. 1
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
4-Phenoxybutoxy-substituted heterocycles-A structure-activity relationship study of blockers of the lymphocyte potassium channel Kv1. 3
Bodendiek SB, et al.
European Journal of Medicinal Chemistry, 44(5), 1838-1852 (2009)
Identification of phase-I metabolites and chronic toxicity study of the Kv1. 3 blocker PAP-1 (5-(4-phenoxybutoxy) psoralen) in the rat
Hao B, et al.
Xenobiotica, 41(3), 198-211 (2011)
Dai-Chao Ma et al.
Experimental neurology, 332, 113399-113399 (2020-07-12)
After cerebral ischemia/reperfusion injury, pro-inflammatory M1-like and anti-inflammatory M2-like phenotypes of microglia are involved in neuroinflammation, in which NLRP3 inflammasome plays an essential role. Kv1.3 channel has been recognized as neuro-immunomodulatory target, but it is not clear as to its
Joaquim Bobi et al.
Translational research : the journal of laboratory and clinical medicine, 224, 40-54 (2020-06-12)
The modulation of voltage-gated K+ (Kv) channels, involved in cell proliferation, arises as a potential therapeutic approach for the prevention of intimal hyperplasia present in in-stent restenosis (ISR) and allograft vasculopathy (AV). We studied the effect of PAP-1, a selective
Alicia de la Cruz et al.
Frontiers in pharmacology, 8, 177-177 (2017-04-15)
Fludarabine (F-ara-A) is a purine analog commonly used in the treatment of indolent B cell malignancies that interferes with different aspects of DNA and RNA synthesis. K
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