A K2P3.1/TASK1 inhibitor
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A-1899

Item No. 43018

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(2,4-difluorophenyl)methyl]-2′-[[[2-(4-methoxyphenyl)acetyl]amino]methyl]-[1,1′-biphenyl]-2-carboxamide
CAS Number
498577-46-1
Synonyms
  • S-20951
Molecular Formula
C30H26F2N2O3
Formula Weight
500.5
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
O=C(NCC1=CC=C(C=C1F)F)C2=C(C=CC=C2)C3=C(CNC(CC4=CC=C(C=C4)OC)=O)C=CC=C3
InChi Code
InChI=1S/C30H26F2N2O3/c1-37-24-14-10-20(11-15-24)16-29(35)33-18-21-6-2-3-7-25(21)26-8-4-5-9-27(26)30(36)34-19-22-12-13-23(31)17-28(22)32/h2-15,17H,16,18-19H2,1H3,(H,33,35)(H,34,36)
InChi Key
IXKPEYHRIVQTCU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

    5 mg

    $39

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    10 mg

    $59

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    25 mg

    $97

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    50 mg

    $136

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    Product Description

    A-1899 is an inhibitor of the two-pore domain potassium channel 3.1 (K2P3.1/TASK1; IC50 = 0.035 µM in Xenopus oocytes expressing the human channel).1 It is selective for K2P3.1/TASK1 over K2P5.1/TASK2, K2P9.1/TASK3, and K2P17.1/TASK4 (IC50s = 12, 0.318, and 8.1 µM, respectively) and a panel of 16 additional potassium channels at 0.1 µM. A-1899 (3 mg/kg) selectively increases the effective refractory period (ERP) in the left atrium over the right atrium and does not affect ventricular repolarization in anesthetized pigs.2 It stimulates breathing and induces respiratory alkalosis in spontaneously breathing anesthetized rats when administered at a dose of 25 mg/kg.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Streit, A.K., Netter, M.F., Kempf, F., et al. A specific two-pore domain potassium channel blocker defines the structure of the TASK-1 open pore. The Journal of Biological Chemisty 286(16), 13977-13984 (2011).

    2. Knobloch, K., Brendel, J., Peukert, S., et al. Electrophysiological and antiarrhythmic effects of the novel IKur channel blockers, S9947 and S20951, on left vs. right pig atrium in vivo in comparison with the IKr blockers dofetilide, azimilide, d,l-sotalol and ibutilide. Naunyn Schmiedebergs Arch Pharmacol. 366(5), 482-487 (2002).

    3. Cotten, J.F. TASK-1 (KCNK3) and TASK-3 (KCNK9) tandem pore potassium channel antagonists stimulate breathing in isoflurane-anesthetized rats. Anesth. Analg. 116(4), 810-816 (2013).