1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor
  3. Zuranolone

Zuranolone 

Cat. No.: HY-103040 Purity: 99.96%
Handling Instructions

Zuranolone est un modulateur du récepteur GABAA qui est allostérique positif stéroïde neuroactif actif et puissant , avec des EC50s de 296 et 163 nM pour α1β2γ2 et récepteur α4β3δ GABAA, respectivement.

Zuranolone is an orally active and potent neuroactive steroid positive allosteric modulator of GABAA receptor, with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.

For research use only. We do not sell to patients.

Zuranolone Chemical Structure

Zuranolone Chemical Structure

CAS No. : 1632051-40-1

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10 mM * 1 mL in DMSO USD 81 In-stock
Estimated Time of Arrival: December 31
2 mg USD 50 In-stock
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5 mg USD 90 In-stock
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10 mg USD 150 In-stock
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25 mg USD 320 In-stock
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50 mg USD 545 In-stock
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100 mg USD 940 In-stock
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200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Zuranolone is an orally active and potent neuroactive steroid positive allosteric modulator of GABAA receptor, with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively[1].

IC50 & Target

EC50: 296 nM (α1β2γ2 GABAA receptor), 163 nM (α4β3δ GABAA receptor)[1]

In Vitro

Zuranolone is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively. Zuranolone is currently being studied in parallel phase 2 clinical trials for the treatment of postpartum depression (PPD) and major depressive disorder (MDD). Zuranolone shows >30 μM inhibition in a cardiac panel of eight relevant cardiac ion channels. At 10 μM concentration of Zuranolone, only binding at the glycine (57%), sigma receptors (88%), and inhibition of the transient receptor potential vanilloid 1 (TRPV1, 95%) is noted[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Acute administration of Zuranolone (0.3 to 10 mg/kg, ip) effectively reduces pentylenetretazol (PTZ)-induced seizures in mice (MECplasma=85 nM) as well as produces a dose-dependent anticonvulsant effect in the mouse 6 Hz electrical stimulation model. In the rat model of status epilepticus (SE), Zuranolone (0.3 to 5 mg, iv) 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 oral bioavailability (F=68%)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

409.56

Formula

C₂₅H₃₅N₃O₂

CAS No.

1632051-40-1

SMILES
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (244.16 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4416 mL 12.2082 mL 24.4164 mL
5 mM 0.4883 mL 2.4416 mL 4.8833 mL
10 mM 0.2442 mL 1.2208 mL 2.4416 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (6.10 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.10 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.10 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

In vivo pharmacokinetic parameters are determined in male Sprague Dawley rats (of 200 to 300 g in weight), male CD-1 mice (15 to 25 g in weight), and male beagle dogs (8 to 12 kg in weight). Doses of Zuranolone for intravenous (IV) and oral administration (PO) are formulated as solutions in SBECD. Zuranolone is dosed IV (5 mg/kg, 2.5 mL/kg) or by oral gavage (20 mg/kg, 10 mL/kg). Animals in the IV group are sampled at 0.083, 0.25, 1, 2, 4, and 8 hours post-dose and PO animals are sampled at 0.5, 1, 2, 4, and 8 hours post dose. Brain samples from the IV group are also collected at 1 hour post-dose. Blood samples are collected into tubes treated with K2-EDTA, then centrifuged at 2000 g at 4°C for 15 min. Plasma is isolated and frozen at -70°C until extraction[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.96%

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Keywords:

ZuranoloneGABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorInhibitorinhibitorinhibit

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