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Soticlestat

Cat. No. M21184
Soticlestat Structure
Synonym:

TAK-935; OV935

Size Price Availability
5mg USD 220  USD220 Out of stock
10mg USD 375  USD375 Out of stock
25mg USD 700  USD700 Out of stock
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Biological Activity

Soticlestat (TAK-935; OV935) is a first-in-class, potent, selective, orally active inhibitor of cholesterol 24-hydroxylase (CH24H), which is used in the study of epilepsy syndromes.

Chemical Information
Molecular Weight 373.45
Formula C23H23N3O2
CAS Number 1429505-03-2
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Cecil D Hahn, et al. Epilepsia. A phase 2, randomized, double-blind, placebo-controlled study to evaluate the efficacy and safety of soticlestat as adjunctive therapy in pediatric patients with Dravet syndrome or Lennox-Gastaut syndrome (ELEKTRA)

[2] Toshiya Nishi, et al. Epilepsia. Anticonvulsive properties of soticlestat, a novel cholesterol 24-hydroxylase inhibitor

[3] Nicole A Hawkins, et al. Epilepsia. Soticlestat, a novel cholesterol 24-hydroxylase inhibitor, reduces seizures and premature death in Dravet syndrome mice

[4] Adam Strzelczyk, et al. CNS Drugs. Expanding the Treatment Landscape for Lennox-Gastaut Syndrome: Current and Future Strategies

[5] Toshiya Nishi, et al. Sci Rep. Soticlestat, a novel cholesterol 24-hydroxylase inhibitor shows a therapeutic potential for neural hyperexcitation in mice

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Keywords: Soticlestat, TAK-935; OV935 supplier, Cytochrome P450 (e.g. CYP17), inhibitors, activators

 
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