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Submit ReviewPenitrem A
Description: Potent and selective KCa1.1 (BK) channel blocker
Chemical Name: 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
Purity: ≥95% (HPLC)
Biological Activity 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.
Technical Data for Penitrem A
| M. Wt | 634.2 |
| Formula | C37H44ClNO6 |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Penitrem A
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 6.34 | 10 |
Preparing Stock Solutions for Penitrem A
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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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Product Datasheets for Penitrem A
References for Penitrem A
References are publications that support the biological activity of the product.
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.
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Keywords: 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 Citations for Penitrem A
Citations are publications that use Tocris products. Selected citations for Penitrem A include:
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
Do you know of a great paper that uses Penitrem A from Tocris? Please let us know.
Reviews for Penitrem A
Average Rating: 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
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: 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.
