A blocker of KCNQ channels
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XE 991 (hydrochloride)

Item No. 14582

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone, dihydrochloride
CAS Number
122955-13-9
Molecular Formula
C26H20N2O • 2HCl
Formula Weight
449.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 2 mg/ml
SMILES
O=C1C2=C(C=CC=C2)C(CC3=CC=NC=C3)(CC4=CC=NC=C4)C5=C1C=CC=C5.Cl.Cl
InChi Code
InChI=1S/C26H20N2O.2ClH/c29-25-21-5-1-3-7-23(21)26(17-19-9-13-27-14-10-19,18-20-11-15-28-16-12-20)24-8-4-2-6-22(24)25;;/h1-16H,17-18H2;2*1H
InChi Key
WOGWMARIFDNZON-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $69

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    10 mg

    $127

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    50 mg

    $525

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    Product Description

    The KCNQ potassium channels are neuronal modulators which combine with other KQT or KCNE channels to form heteromultimers. XE 991 is a blocker of KCNQ channels that potently inhibits KCNQ1 and 2 homomeric channels (IC50 = 0.75 and 0.71 µM, respectively) as well as KCNQ2+3 heteromultimers (IC50 = 0.6 µM).1 It much less effectively blocks eag, erg, and elk channels. The effectiveness of XE 991 against KCNQ channels depends on partners or accessory proteins.2 Through these actions, XE 991 enhances acetylcholine release from rat brain slices (EC50 = 490 nM) and shows good in vivo potency and duration of action, suggesting utility in Alzheimer’s disease therapeutics.3 While early studies focused on actions in the central nervous system, XE 991 can be used to explore the roles of KCNQ channels in neuronal regulation throughout the body.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, H.S., Pan, Z., Shi, W., et al. KCNQ2 and KCNQ3 potassium channel subunits: Molecular correlates of the M-channel. Science 282(5395), 1890-1893 (1998).

    2. Wang, H.S., Brown, B.S., McKinnon, D., et al. Molecular basis for differential sensitivity of KCNQ and IKs channels to the cognitive enhancer XE991. Mol. Pharmacol. 57(6), 1218-1223 (2000).

    3. Zaczek, R., Chorvat, R.J., Saye, J.A., et al. Two new potent neurotransmitter release enhancers, 10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone and 10,10-bis(2-fluoro-4-pyridinylmethyl)-9(10H)-anthracenone: Comparison to linopirdine. J. Pharmacol. Exp. Ther. 285(2), 724-730 (1998).

    4. Hawryluk, J.M., Moreira, T.S., Takakura, A.C., et al. KCNQ channels determine serotonergic modulation of ventral surface chemoreceptors and respiratory drive. J. Neurosci. 32(47), 16943-16952 (2012).