Penitrem A

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Cat.No. 4617 - Penitrem A | C37H44ClNO6 | CAS No. 12627-35-9
Description: Potent and selective BKCa (KCa1.1) 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: ≥98% (HPLC)
Datasheet
Citations (3)
Reviews (1)
Literature (2)

Biological Activity

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

M. Wt 634.2
Formula C37H44ClNO6
Storage Store at -20°C
Purity ≥98% (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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 6.34 10

Preparing Stock Solutions

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

Certificate of Analysis / Product Datasheet
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References

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


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View all Calcium-Activated Potassium (KCa) Channel Blockers

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:

Abrahao et al (2017) Ethanol-Sensitive Pacemaker Neurons in the Mouse External Globus Pallidus. Neuropsychopharmacology 42 1070 PMID: 27827370

Khan et al (2019) BK channels regulate extracellular Tat-mediated HIV-1 LTR transactivation. Sci Rep 9 12285 PMID: 31439883

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


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Reviews for 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.

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