A KCa2.1/SK1 activator
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GW 542573X

Item No. 43213

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[[[(2-methoxyphenyl)amino]carbonyl]oxy]methyl]-1-piperidinecarboxylic acid, 1,1-dimethylethyl ester
CAS Number
660846-41-3
Molecular Formula
C19H28N2O5
Formula Weight
364.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/mlPBS (pH 7.2): Soluble: ≥10 mg/ml
SMILES
O=C(NC1=C(C=CC=C1)OC)OCC2CCN(CC2)C(OC(C)(C)C)=O
InChi Code
InChI=1S/C19H28N2O5/c1-19(2,3)26-18(23)21-11-9-14(10-12-21)13-25-17(22)20-15-7-5-6-8-16(15)24-4/h5-8,14H,9-13H2,1-4H3,(H,20,22)
InChi Key
SAXGSDIZIYFNKD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $39

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    5 mg

    $174

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    10 mg

    $251

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    25 mg

    $578

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    Product Description

    GW 542573X is an activator of small-conductance calcium-activated potassium channel KCa2.1/SK1.1 It increases current in an inside-out patch clamp assay using HEK293 cells expressing the human channel (EC50 = 8.2 µM). GW 542573X is selective for KCa2.1/SK1 over KCa2.2/SK2, KCa2.3/SK3, and intermediate-conductance calcium-activated potassium channel KCa3.1/IK in whole-cell patch clamp assays using HEK293 cells expressing the human channels at 10 µM, as well as the voltage-gated sodium channel Nav1.3, N-type voltage-gated calcium channel Cav2.2, voltage-gated potassium channel Kv1.3, purinergic P2X2/3 receptor, and α7 nicotinic acetylcholine receptor (nAChR) at 30 µM. In vivo, GW 542573X (15 mg/kg) decreases freezing time in contextual fear but not cued fear memory tests in mice when administered prior to the conditioning period.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hougaard, C., Jensen, M.L., Dale, T.J., et al. Selective activation of the SK1 subtype of human small-conductance Ca2+-activated K+ channels by 4-(2-methoxyphenylcarbamoyloxymethyl)-piperidine-1-carboxylic acid tert-butyl ester (GW542573X) is dependent on serine 293 in the S5 segment. Mol. Pharmacol. 76(3), 569-578 (2009).

    2. Rice, C.A., and Stackman, R.W., Jr. The small conductance Ca2+-activated K+ channel activator GW542573X impairs hippocampal memory in C57BL/6J mice. Neuropharmacology 252:109960, (2024).