Paxilline

Pricing Availability Delivery Time Qty
Cat.No. 2006 - Paxilline | C27H33NO4 | CAS No. 57186-25-1
Description: SERCA ATPase blocker. Also potent BKCa channel blocker
Chemical Name: (2R,4bS,6aS,12bS,12cR,14aS)-5,6,6a,7,12,12b,12c,13,14,14a-Decahydro-4b-hydroxy-2-(1-hydroxy-1-methylethyl)-12b,12c-dimethyl-2H-pyrano[2'',3'':5',6']benz[1',2':6,7]indeno[1,2-b]indol-3(4bH)-one
Purity: ≥98% (HPLC)
Datasheet
Citations (7)

Biological Activity

Potent blocker of high-conductance Ca2+-activated K+ (BKCa, KCa1.1) channels. Binds to the α-subunit of BKCa (Ki = 1.9 nM for block of currents in α-subunit-expressing oocytes) and enhances binding of charybdotoxin to BKCa channels in vascular smooth muscle. Also inhibits sarco/endoplasmic reticulum Ca2+-ATPase (IC50 = 5 - 50 μM).

Technical Data

M. Wt 435.56
Formula C27H33NO4
Storage Desiccate at -20°C
Purity ≥98% (HPLC)
CAS Number 57186-25-1
PubChem ID 105008
InChI Key ACNHBCIZLNNLRS-UBGQALKQSA-N
Smiles [H][C@@]4([C@](C)3[C@]5(C)[C@@](C([C@]6([H])CC5)=CC([C@@H]([C@](O)(C)C)O6)=O)(O)CC4)CC2=C3NC1=CC=CC=C12

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 43.56 100
ethanol 8.71 20

Preparing Stock Solutions

The following data is based on the product molecular weight 435.56. 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 2.3 mL 11.48 mL 22.96 mL
5 mM 0.46 mL 2.3 mL 4.59 mL
10 mM 0.23 mL 1.15 mL 2.3 mL
50 mM 0.05 mL 0.23 mL 0.46 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.

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

Sanchez and McManus (1996) Paxilline inhibition of the alpha-subunit of the high-conductance calcium-activated potassium channel. Neuropharmacology 35 963 PMID: 8938726

Bilmen et al (2002) The mechanism of inhibition of the sarco/endoplasmic reticulum Ca2+ ATPase by paxilline. Arch.Biochem.Biophys. 406 55 PMID: 12234490


If you know of a relevant reference for Paxilline, please let us know.

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Keywords: Paxilline, supplier, Potent, blockers, BKCa, channels, SERCA, ATPases, Potassium, ca2+-activated, ca2+-dependent, Ca2+-ATPase, Signaling, Signalling, Calcium, Calcium-ATPase, Ion, Transporters, Pumps, Ca2+-Activated, Potassium, Channels, Ca2+-ATPase, Ca2+-ATPase, Tocris Bioscience

7 Citations for Paxilline

Citations are publications that use Tocris products. Selected citations for Paxilline include:

Hirono et al (2015) BK Channels Localize to the Paranodal Junction and Regulate Action Potentials in Myelinated Axons of Cerebellar Purkinje Cells. J Neurosci 35 7082 PMID: 25948259

Kim et al (2015) Astrocyte contributions to flow/pressure-evoked parenchymal arteriole vasoconstriction. J Neurophysiol 35 8245 PMID: 26019339

Lai et al (2014) BK channels regulate sinoatrial node firing rate and cardiac pacing in vivo. Am J Physiol Heart Circ Physiol 307 H1327 PMID: 25172903

Montgomery et al (2013) Mis-expression of the BK K(+) channel disrupts suprachiasmatic nucleus circuit rhythmicity and alters clock-controlled behavior. Am J Physiol Cell Physiol 304 C299 PMID: 23174562

Wan et al (2013) Reduced vascular smooth muscle BK channel current underlies heart failure-induced vasoconstriction in mice. Nat Commun 27 1859 PMID: 23325318

Gittis et al (2010) Mechanisms of sustained high firing rates in two classes of vestibular nucleus neurons: differential contributions of resurgent Na, Kv3, and BK currents. J Neurosci 104 1625 PMID: 20592126

Pyott et al (2004) Extrasynaptic localization of inactivating calcium-activated potassium channels in mouse inner hair cells. FASEB J 24 9469 PMID: 15509733


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