Paxilline |
| Catalog No.: GC11082 |
High-conductance Ca2+-activated K+ (BKCa, KCa1.1) channels blocker
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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).
| Cas No. | 57186-25-1 | SDF | |
| Synonyms | N/A | ||
| Chemical Name | (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 | ||
| Formula | C27H33NO4 | M.Wt | 435.56 |
| Solubility | 10mg/mL in ethanol, 30mg/mL in DMSO, or in DMF | Storage | 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 |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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