Penitrem A

Pricing Availability Delivery Time Qty
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 (1)
Literature

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.

All Tocris products are intended for laboratory research use only.

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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.58 mL 7.88 mL 15.77 mL
5 mM 0.32 mL 1.58 mL 3.15 mL
10 mM 0.16 mL 0.79 mL 1.58 mL
50 mM 0.03 mL 0.16 mL 0.32 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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: PenitremA maxi-k bk channels potent selective inhibitors inhibits blockers slo KCa KCa1.1 K+ high conductance Ca2+-dependent Potassium Ca2+-activated Ca2+-dependent Ca2+-Activated Potassium Channels

1 Citation 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


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