A cholesterol 24-hydroxylase/CYP46A1 inhibitor
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Soticlestat

Item No. 34928

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
[2,4′-bipyridin]-3-yl[4-hydroxy-4-(phenylmethyl)-1-piperidinyl]-methanone
CAS Number
1429505-03-2
Synonyms
  • OV935
  • TAK-935
Molecular Formula
C23H23N3O2
Formula Weight
373.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
SMILES
O=C(N1CCC(CC2=CC=CC=C2)(CC1)O)C3=C(C4=CC=NC=C4)N=CC=C3
InChi Code
InChI=1S/C23H23N3O2/c27-22(20-7-4-12-25-21(20)19-8-13-24-14-9-19)26-15-10-23(28,11-16-26)17-18-5-2-1-3-6-18/h1-9,12-14,28H,10-11,15-17H2
InChi Key
XKUZMIUSBMCVPP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    500 µg

    $57

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    1 mg

    $102

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    5 mg

    $223

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    10 mg

    $418

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    Product Description

    Soticlestat is an inhibitor of cholesterol 24-hydroxylase/CYP46A1 (IC50 = 0.0074 µM).1 It is selective for cholesterol 24-hydroxylase/CYP46A1 over the cytochrome P450 (CYP) isoforms CYP2C8, -2C9, -2D6, -3A4, -1A2, and 2C19 (IC50s = 62, 19, >100, 66, >100, and 14 µM, respectively). Soticlestat (0.02% in the diet) reduces seizure frequency and severity and improves survival in a model of Dravet syndrome induced by hyperthermia in mice with heterozygous deletion of Scn1a (Scn1a+/-), the gene encoding voltage-gated sodium channel 1.1 (Nav1.1).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Koike, T., Yoshikawa, M., Ando, H.K., et al. Discovery of soticlestat, a potent and selective inhibitor for cholesterol 24-hydroxylase (CH24H). J. Med. Chem. 64(16), 12228-12244 (2021).

    2. Hawkins, N.A., Jurado, M., Thaxton, T.T., et al. Soticlestat, a novel cholesterol 24-hydroxylase inhibitor, reduces seizures and premature death in Dravet syndrome mice. Epilepsia 62(11), 2845-2857 (2021).