An agonist of α4β2 nAChRs
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Sofiniclin

Item No. 46219

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1S)-3-(5S,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane
CAS Number
799279-80-4
Synonyms
  • ABT-894
Molecular Formula
C10H11Cl2N3
Formula Weight
244.1
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
ClC1=CC(N2C[C@@]3([H])[C@@](NC3)([H])C2)=CN=C1Cl
InChi Code
InChI=1S/C10H11Cl2N3/c11-8-1-7(3-14-10(8)12)15-4-6-2-13-9(6)5-15/h1,3,6,9,13H,2,4-5H2/t6-,9+/m0/s1
InChi Key
MBQYQLWSBRANKQ-IMTBSYHQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $139

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    1 mg

    $250

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    5 mg

    $626

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    10 mg

    $973

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    Product Description

    Sofiniclin is an agonist of α4β2 nicotinic acetylcholine receptors (nAChRs).1 It induces activation of high- and low-sensitivity α4β2 nAChRs in membrane potential assays (EC50s = 3 and 17 nM, respectively) and desensitization of the same receptors with half-maximal desensitization concentration (DC50) values of 11 and 49 nM, respectively, in membrane potential assays. Sofiniclin selectively binds to α4β2 nAChRs over α3β4 and α7 nAChRs (Kis = 0.9, 180, and 750 nM, respectively, for the human receptors), and it also binds to α6β2 nAChRs (Ki = 1.9 nM).1,2 It induces analgesia in the first and second phase of the formalin test in mice at 3 mg/kg.1 Sofiniclin inhibits levodopa-induced dyskinesias in a squirrel monkey model of Parkinson’s disease.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhang, J., Xiao, Y.-D., Jordan, K.G., et al. Analgesic effects mediated by neuronal nicotinic acetylcholine receptor agonists: Correlation with desensitization of α4β2* receptors. Eur. J. Pharm. Sci. 47(5), 813-823 (2012).

    2. Zhang, D., Bordia, T., McGregor, M., et al. ABT-089 and ABT-894 reduce levodopa-induced dyskinesias in a monkey model of Parkinson’s disease. Mov. Disord. 29(4), 508-517 (2014).