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Zuranolone

Cat. No. M10326
Zuranolone Structure
Synonym:

SAGE-217; CS-2797

Size Price Availability Quantity
5mg USD 85.5  USD95 In stock
10mg USD 138.6  USD154 In stock
25mg USD 289.8  USD322 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Zuranolone also known as SAGE-217, is a potent GABAA receptor agonist with EC50 values of 296 nM and 163 nM for α1β2γ2 and α4β3δ GABAA receptors. Zuranolone shows >30 μM inhibition in a cardiac panel of eight relevant cardiac ion channels. In vivo, Zuranolone (0.3-5 mg/kg, i.v.) in the rat model of status epilepticus (SE) abolishes both behavioral and electrographic seizure activity, even when administered 60 min after induction of SE. Additional PK studies of Zuranolone in dog show low clearance (<10% of hepatic blood flow), resulting in excellent 68% oral bioavailability.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 409.56
Formula C25H35N3O2
CAS Number 1632051-40-1
Purity >99%
Solubility DMSO 82 mg/mL
Storage at -20°C
References

Preclinical characterization of zuranolone (SAGE-217), a selective neuroactive steroid GABA A receptor positive allosteric modulator
Alison L Althaus, et al. Neuropharmacology. 2020 Dec 15;181:108333. PMID: 32976892.

Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid) A Receptor
Gabriel Martinez Botella, et al. J Med Chem. 2017 Sep 28;60(18):7810-7819. PMID: 28753313.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Zuranolone, SAGE-217; CS-2797 supplier, GABA Receptor, inhibitors

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