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Submit ReviewPenitrem A
说明： Potent and selective KCa1.1 (BK) channel blocker
化学名： 2R,3S,3aR,4aS,4bS,6aR,7S,7dR,8R,9aR,14bS,14cR,16aS)-12-chloro-3,3a,6a,8,9,9a,10,11,14,14b,14c,15,16,16a-tetradecahydro-14b,14c,17,17-tetramethyl-10-methylene-2-(1-methylethenyl)-7,8-(epoxymethano)-2H,6H-cyclobuta[5,6]benz[1,2-e]oxireno[4',4'a]-1-benzopyrano[5',6':6,7]indeno[1,2-b]indole-3,4b,7d(5H,7H)-triol
纯度： ≥95% (HPLC)
生物活性 for Penitrem A
Penitrem A is a potent and selective blocker of BKCa (KCa1.1) channels (IC50 values are 6.4 and 64.4 nM for BKCa channels containing α subunits only, and those containing α and β1 respectively). Displays no effect on native delayed rectifier K+ and KATP currents, or cloned KV1.5 channels. Blocks BKCa channels in both inside-out and cell-attached patches. Shown to enhance smooth muscle contraction in vitro and increase total peripheral resistance in vivo.
技术数据 for Penitrem A
| 分子量 | 634.2 |
| 公式 | C37H44ClNO6 |
| 储存 | Store at -20°C |
| 纯度 | ≥95% (HPLC) |
| CAS Number | 12627-35-9 |
| PubChem ID | 6610243 |
| InChI Key | JDUWHZOLEDOQSR-JKPSMKLGSA-N |
| Smiles | O[C@H]9[C@@H]([C@](C)=C)O[C@@]([C@@]%108[C@@H]9O%10)([H])CC[C@]([C@@]8(O)CC7)(C)[C@@]([C@]7([H])[C@@H]4OC(C)(C)[C@]([H])5C6)(C)C3=C4C1=C(N3)C=C(Cl)C2=C1[C@@]5(O)[C@@]6([H])C(C2)=C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Penitrem A
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 6.34 | 10 |
制备储备液 for Penitrem A
以下数据基于产品分子量 634.2。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 15.77 mL | 78.84 mL | 157.68 mL |
| 0.5 mM | 3.15 mL | 15.77 mL | 31.54 mL |
| 1 mM | 1.58 mL | 7.88 mL | 15.77 mL |
| 5 mM | 0.32 mL | 1.58 mL | 3.15 mL |
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产品说明书 for Penitrem A
参考文献 for Penitrem A
参考文献是支持产品生物活性的出版物。
Asano et al (2012) Penitrem A as a tool for understanding the role of large conductance Ca2+/voltage-sensitive K+ channels in vascular function. J.Pharmacol.Exp.Ther. 342 453 PMID: 22580348
Knaus et al (1994) Tremorgenic indole alkaloids potently inhibit smooth muscle high-conductance calcium-activated potassium channels. Biochemistry 33 5819 PMID: 7514038
If you know of a relevant reference for Penitrem A, please let us know.
关键词: Penitrem A, Penitrem A supplier, PenitremA, maxi-k, bk, channels, potent, selective, inhibitors, inhibits, blockers, slo, KCa, KCa1.1, K+, high, conductance, Ca2+-dependent, Potassium, Ca2+-activated, Ca2+-Activated, Channels, 4617, Tocris Bioscience
3 篇 Penitrem A 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Penitrem A 的部分引用包括：
Hirono et al (2015) BK Channels Localize to the Paranodal Junction and Regulate Action Potentials in Myelinated Axons of Cerebellar Purkinje Cells. J Biol Chem 35 7082 PMID: 25948259
Khan et al (2019) BK channels regulate extracellular Tat-mediated HIV-1 LTR transactivation. Sci Rep 9 12285 PMID: 31439883
Abrahao et al (2017) Ethanol-Sensitive Pacemaker Neurons in the Mouse External Globus Pallidus. Neuropsychopharmacology 42 1070 PMID: 27827370
您是否知道使用了 Tocris Penitrem A 的优秀论文？ 请告知我们.
Penitrem A 的评论
平均评分: 4 (Based on 1 Review.)
Have you used Penitrem A?
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Penitrem A as a selective BK blocker worked ideally.
By
Sadequl Islam on 10/13/2018
分析类型： In Vitro
种属： Human
细胞系/组织： HEK 293
Product used to understand BK channel blocking activity on HEK 293 cell line.The cell line expresses brain alpha subunits of BK channel. Showed blocking activity on electrophysiological tests. Product worked ideally and would definitely worth buying.
