CAS NO: | 1632051-40-1 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
2mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Zuranolone is an orally active and potent neuroactive steroid positive allosteric modulator ofGABAAreceptor, withEC50s of 296 and 163 nM forα1β2γ2andα4β3δ GABAAreceptors, respectively[1]. | ||||||||||||||||
IC50& Target | EC50: 296 nM (α1β2γ2GABAAreceptor), 163 nM (α4β3δ GABAAreceptor)[1] | ||||||||||||||||
体外研究 (In Vitro) | Zuranolone is a potent GABAAreceptor agonist with EC50s of 296 and 163 nM for α1β2γ2and α4β3δ GABAAreceptors, 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]. | ||||||||||||||||
体内研究 (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]. | ||||||||||||||||
分子量 | 409.56 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C25H35N3O2 | ||||||||||||||||
CAS 号 | 1632051-40-1 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(244.16 mM;Need ultrasonic) H2O :< 0.1 mg/mL(insoluble) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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