An inhibitor of K2P3.1/TASK1
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AVE-1231

Item No. 45299

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(butylsulfonyl)amino]-N-[(1R)-1-(6-methoxy-3-pyridinyl)propyl]-benzamide
CAS Number
767334-89-4
Synonyms
  • A293
Molecular Formula
C20H27N3O4S
Formula Weight
405.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile:Water (1:1): Slightly soluble: 0.1-1 mg/mlDMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
CC[C@H](C1=CN=C(OC)C=C1)NC(C(C=CC=C2)=C2NS(CCCC)(=O)=O)=O
InChi Code
InChI=1S/C20H27N3O4S/c1-4-6-13-28(25,26)23-18-10-8-7-9-16(18)20(24)22-17(5-2)15-11-12-19(27-3)21-14-15/h7-12,14,17,23H,4-6,13H2,1-3H3,(H,22,24)/t17-/m1/s1
InChi Key
BFQMQSIBOHOPCY-QGZVFWFLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $299

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    5 mg

    $748

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    10 mg

    $1,047

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    Product Description

    AVE-1231 is an inhibitor of two-pore domain potassium channel 3.1 (K2P3.1), also known as TWIK-related acid-sensitive potassium channel (TASK1).1 It reduces potassium currents in X. laevis oocytes expressing TASK1 (IC50 = 0.22 µM) but also those expressing voltage-gated potassium channel 1.5 (Kv1.5; IC50 = 5.6 µM).2 AVE-1231 (1 mg/kg) restores sinus rhythm in a porcine model of acute paroxysmal atrial fibrillation.3 It also reduces the severity of experimental autoimmune encephalomyelitis (EAE) in wild-type mice but not TASK1 knockout mice when administered at a dose of 0.02 mg/kg.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Shvetsova, A.A., Lazarenko, V.S., Gaynullina, D.K., et al. TWIK-related acid-sensitive potassium channels (TASK-1) emerge as contributors to tone regulation in renal arteries at alkaline pH. Front. Physiol. 13, 895863 (2022).

    2. Kiper, A.K., Rinné, S., Rolfes, C., et al. Kv1.5 blockers preferentially inhibit TASK-1 channels: TASK-1 as a target against atrial fibrillation and obstructive sleep apnea? Pflugers. Arch. 467(5), 1081-1090 (2015).

    3. Wiedmann, F., Beyersdorf, C., Zhou, X., et al. Pharmacologic TWIK-related acid-sensitive K+ channel (TASK-1) potassium channel inhibitor A293 facilitates acute cardioversion of paroxysmal atrial fibrillation in a porcine large animal model. J. Am. Heart Assoc. 9(10), e015751 (2020).

    4. Bittner, S., Bauer, M.A., Ehling, P., et al. The TASK1 channel inhibitor A293 shows efficacy in a mouse model of multiple sclerosis. Exp. Neurol. 238(2), 149-155 (2012).