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.
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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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
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