| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
This product is discontinued due to commercial reason. Zuranolone (formerly known as SAGE-217; SAGE217; Zurzuvae) is an investigational drug being developed for the treatment of depressive disorders. It acts as a novel and potent GABAA receptor modulator/agonist at both synaptic and extrasynaptic receptor subtypes with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively, and with excellent oral DMPK properties. SAGE-217 has completed a phase 1 single ascending dose (SAD) and multiple ascending dose (MAD) clinical trial and is currently being studied in parallel phase 2 clinical trials for the treatment of postpartum depression (PPD), major depressive disorder (MDD), and essential tremor (ET). Certain classes of neuroactive steroids (NASs) are positive allosteric modulators (PAM) of synaptic and extrasynaptic GABAA receptors. Zuranolone (Zurzuvae) was approved in 2023 by FDA for treating Postpartum depression.
| ln Vitro |
With EC50s of 296 and 163 nM for α1β2η2 and α4β3δ GABAA receptors, respectively, zuranolone is a strong agonist of GABAA receptors. Phase 2 clinical trials investigating zuranolone are presently being conducted in parallel to treat major depressive disorder (MDD) and postpartum depression (PPD). In a cardiac panel consisting of eight significant cardiac ion channels, zuranolone exhibits >30 μM inhibition. Only binding at the glycine (57%), sigma (88%), and transient receptor potential vanilloid 1 (TRPV1, 95%) is observed at 10 μM concentration of Zuranolone[1].
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| ln Vivo |
Pentylenetretazol (PTZ)-induced seizures in mice (MECplasma=85 nM) are effectively reduced by acute administration of Zuranolone (0.3 to 10 mg/kg, ip). In addition, a dose-dependent anticonvulsant effect is produced in the mouse 6 Hz electrical stimulation model. Even when given 60 minutes after the onset of status epilepticus (SE), Zuranolone (0.3 to 5 mg, iv) completely eliminates both behavioral and electrographic seizure activity in the rat model of SE. Further PK studies on dogs with Zuranolone demonstrate excellent oral bioavailability (F=68%) due to low clearance (< 10% of hepatic blood flow)[1].
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| References |
[1]. Martinez Botella G, et al. Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5β-pregnan-20-one: A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)A Receptor. J Med Chem. 2017 Sep 28;60(18):7810-7819
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| Molecular Formula |
C25H35N3O2
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| Molecular Weight |
409.57
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| CAS # |
1632051-40-1
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| Related CAS # |
1632051-40-1;DXN51401;
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| SMILES |
O[C@]1(C)CC[C@H]2[C@@H](C1)CC[C@@H]1[C@@H]2CC[C@]2(C)[C@@H](C(CN3C=C(C#N)C=N3)=O)CC[C@@H]12
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| Chemical Name |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.10 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2.5 mg/mL (6.10 mM) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (6.10 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4416 mL | 12.2079 mL | 24.4159 mL | |
| 5 mM | 0.4883 mL | 2.4416 mL | 4.8832 mL | |
| 10 mM | 0.2442 mL | 1.2208 mL | 2.4416 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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