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Paxilline 目录号 GC11082

high-conductance Ca2+-activated K+ (BKCa, KCa1.1) channels blocker

规格 价格 库存 购买数量
1mg
¥468.00
现货
5mg
¥1,287.00
现货
10mg
¥2,340.00
现货

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 57186-25-1 SDF
别名 N/A
化学名 (2R,4bS,6aR,12bS,12cR,14aS)-4b-hydroxy-2-(2-hydroxypropan-2-yl)-12b,12c-dimethyl-5,6,6a,7,12,12b,12c,13,14,14a-decahydro-2H-chromeno[5',6':6,7]indeno[1,2-b]indol-3(4bH)-one
Canonical SMILES O[C@]1(C2=C3)[C@@](CC[C@@H]2O[C@H](C(C)(C)O)C3=O)(C)[C@](C(NC4=CC=CC=C54)=C5C6)(C)[C@@H]6CC1
分子式 C27H33NO4 分子量 435.56
溶解度 10mg/mL in ethanol, 30mg/mL in DMSO, or in DMF 储存条件 Desiccate at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

产品描述

Paxilline is an indole diterpene from fungi which potently and reversibly inhibits large conductance Ca2+-activated K+ (BKCa) channels, as shown in patch clamp (Ki = 1.9 nM) and whole smooth muscle cell studies (Ki = 35.7 nM).[1],[2]It also enhances the binding of charybdotoxin, a peptidyl neurotoxin, to BKCa channels.[3] Paxilline is currently used to evaluate the role of BKCa channels in various cell processes and responses.[4],[5]

Reference:
[1]. Sanchez, M., and McManus, O.B. Paxilline inhibition of the alpha-subunit of the high-conductance calcium-activated potassium channel. Neuropharmacology 35(7), 963-968 (1996).
[2]. Li, G., and Cheung, D.W. Effects of paxilline on K+ channels in rat mesenteric arterial cells. European Journal of Pharmacology 372, 103-107 (1999).
[3]. Knaus, H.G., McManus, O.B., Lee, S.H., et al. Tremorgenic indole alkaloids potently inhibit smooth muscle high-conductance calcium-activated potassium channels. Biochemistry 33(19), 5819-5828 (1994).
[4]. Jackson-Weaver, O., Paredes, D.A., Gonzalez Bosc, L.V., et al. Intermittent hypoxia in rats increases myogenic tone through loss of hydrogen sulfide activation of large-conductance Ca2+-activated potassium channels. Circulation Research 108(12), 1439-1447 (2011).
[5]. Tajima, N., Itokazu, Y., Korpi, E.R., et al. Activity of BKCa channel is modulated by membrane cholesterol content and association with Na+/K+-ATPase in human melanoma IGR39 cells. The Journal of Biological Chemisty 286(7), 5624-5638 (2011).