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Penitrem A

Cat. No. 4617

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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

Biological Activity

Potent and selective blocker of BK_Ca (K_Ca1.1) channels (IC₅₀ values are 6.4 and 64.4 nM for BK_Ca channels containing α subunits only, and those containing α and β1 respectively). Displays no effect on native delayed rectifier K⁺ and K_ATP currents, or cloned K_V1.5 channels. Blocks BK_Ca 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

Solubility:

Soluble to 10 mM in DMSO

Purity:

>98 %

Storage:

Store at -20°C

CAS No:

12627-35-9

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Knaus et al (1994) Tremorgenic indole alkaloids potently inhibit smooth muscle high-conductance calcium-activated potassium channels. Biochemistry 33 5819. PMID: 7514038.

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.

If you know of a relevant citation for this product please let us know.

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Keywords: Penitrem A, supplier, PenitremA, maxi-k, bk, channels, potent, selective, inhibitors, blockers, slo, KCa, KCa1.1, K+, high, conductance, Ca2+-dependent, Potassium, Ca2+-activated, Ca2+-dependent

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