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盐酸鲁拉西酮  ≥98%

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包装规格：5mg 10mg 50mg 100mg in glass bottle
产品简介：Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) 是 dopamine D2 和 5-HT7 的拮抗剂，IC50 值分别为 1.68 和 0.495 nM。 Lurasidone 也是 5-HT1A 受体的部分激动剂，IC50 值为 6.75 nM。
溶解性：DMSO :6.67 mg/mL (12.61 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to) Ethanol：2 mg/mL (3.78 mM; Need ultrasonic) Water：< 0.1 mg/mL (insoluble)
储备液保存：-80°C, 6 months -20°C, 1 month (sealed storage, away from moisture and light)
体内实验：1、请依序添加每种溶剂： 10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility: ≥ 0.67 mg/mL (1.27 mM); Clear solution 此方案可获得 ≥ 0.67 mg/mL (1.27 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 6.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2、请依序添加每种溶剂： 10% DMSO→ 90% (20% SBE-β-CD in saline) Solubility: ≥ 0.67 mg/mL (1.27 mM); Clear solution 此方案可获得 ≥ 0.67 mg/mL (1.27 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 6.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 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。
靶点：5-HT7 Receptor:0.495 nM (IC50) 5-HT1A Receptor:6.75 nM (IC50) D2 Receptor:1.68 nM (IC50)
体外研究：Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of dopamine D2 and 5-HT7 with IC50s of 1.68±0.09 and 0.495±0.090 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75±0.97 nM. In vitro receptor binding experiments reveal that Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) demonstrates affinity for dopamine D2 and 5-HT2A receptors higher than other tested antipsychotics. Lurasidone does not increase [35S]GTPγS binding to the membrane preparations for dopamine D2 receptors by itself, but it antagonizes dopamine-stimulated [35S]GTPγS binding in a concentration-dependent manner with a KB value of 2.8±1.1 nM.
体内研究：Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) dose-dependently increases the ratio of DOPAC/dopamine in both regions, but it shows a preferential effect on the frontal cortex compare with the striatum, especially at higher doses. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) (ED50 values 2.3 to 5.0 mg/kg) shows a comparable potency with olanzapine (ED50 values 1.1 to 5.1 mg/kg), higher potency than clozapine (ED50 9.5 to 290 mg/kg), and slightly lower potency than haloperidol (ED50 values 0.44 to 1.7 mg/kg). Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) (1 to 10 mg/kg) dose-dependently inhibits conditioned avoidance response (CAR) in rats, and the ED50 values are 6.3 mg/kg. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) dose-dependently inhibits TRY-induced forepaw clonic seizure and p-CAMP-induced hyperthermia with ED50 values of 5.6 and 3.0 mg/kg, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) (0.3 to 30 mg/kg) dose-dependently and significantly increases the number of shocks received by rats in the conflict test with MED of 10 mg/kg (p<0.01).
保存条件：2-8°C 密封干燥
注意事项：1、为了您的安全和健康，请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。

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