S86929 |
5-(4-Phenoxybutoxy)psoralen |
源叶(MedMol) | 99% |
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- 产品描述: PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects
- 靶点: EC50: 2 nM (Kv1.3), 45 nM (Kv1.5);PotassiumChannel
- 体内研究:
PAP-1 (0.3-3 mg/kg; i.p.; three times daily for 48 hours) prevents delayed type hypersensitivity (DTH) in lewis rats
- 参考文献:
1. 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. 2. Pereira LE, 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.
- 溶解性: Soluble in DMSO
- 保存条件: 2-8℃,避光
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.854 ml 14.271 ml 28.542 ml 5 mM 0.571 ml 2.854 ml 5.708 ml 10 mM 0.285 ml 1.427 ml 2.854 ml 50 mM 0.057 ml 0.285 ml 0.571 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)