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Lurasidone

Lurasidone

产品编号 T21337   CAS 367514-87-2
别名: SM-13496, 鲁拉西酮

Lurasidone (SM-13496) 是多巴胺 D2和5-HT7的拮抗剂,IC50值分别为 1.68 和 0.495 nM。它也是5-HT1A 受体的部分激动剂,IC50值为 6.75 nM。

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Lurasidone Chemical Structure
Lurasidone, CAS 367514-87-2
规格 价格/CNY 货期 数量
5 mg ¥ 198 现货
10 mg ¥ 333 现货
25 mg ¥ 565 现货
50 mg ¥ 925 现货
100 mg ¥ 1,430 现货
200 mg ¥ 2,130 待询
产品目录号及名称: Lurasidone (T21337)
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纯度: 99.5%
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参考文献
产品描述 Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7(IC50=1.68 and 0.495 nM, respectively).It also a partial agonist of 5-HT1A receptor(IC50 : 6.75 nM).
靶点活性 D2 receptor:1.68 nM (IC50), 5-HT1A receptor:6.75 nM (IC50), 5-HT7 receptor:0.495 nM (IC50)
体外活性 Lurasidone is administered once daily within the range of 40-160 mg/day for schizophrenia and 20-120 mg/day for bipolar depression, and its pharmacokinetic profile requires administration with food.?In adult healthy subjects and patients, a 40 mg dose results in peak plasma concentrations in 1-3 h, a mean elimination half-life of 18 h (mostly eliminated in the feces), and apparent volume of distribution of 6173 L;?it is approximately 99 % bound to serum plasma proteins.?Lurasidone's pharmacokinetics are approximately dose proportional in healthy adults and clinical populations within the approved dosing range, and this was also found in a clinical study of children and adolescents.?Lurasidone is principally metabolized by cytochrome P450 (CYP) 3A4 with minor metabolites and should not be coadministered with strong CYP3A4 inducers or inhibitors.?Lurasidone does not significantly inhibit or induce CYP450 hepatic enzymes[2].
体内活性 In addition to its principal antagonist activity at dopamine D2 and serotonin 5-HT2A receptors, lurasidone has distinctive 5-HT7 antagonistic activity, and displays partial agonism at 5-HT1A receptors, as well as modest antagonism at noradrenergic α2A and α2C receptors.?Lurasidone is devoid of antihistaminic and anticholinergic activities[1].
别名 SM-13496, 鲁拉西酮
分子量 492.68
分子式 C28H36N4O2S
CAS No. 367514-87-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 17.83 mg/mL (36.19 mM), Sonication is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0297 mL 10.1486 mL 20.2972 mL 50.7429 mL
5 mM 0.4059 mL 2.0297 mL 4.0594 mL 10.1486 mL
10 mM 0.203 mL 1.0149 mL 2.0297 mL 5.0743 mL
20 mM 0.1015 mL 0.5074 mL 1.0149 mL 2.5371 mL

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TargetMol Library Books参考文献

1. Greenberg W M , Citrome L . Pharmacokinetics and Pharmacodynamics of Lurasidone Hydrochloride, a Second-Generation Antipsychotic: A Systematic Review of the Published Literature[J]. Clinical Pharmacokinetics, 2016. 2. Maurizio, Pompili, Claudio,et al. Lurasidone: efficacy and safety in the treatment of psychotic and mood disorders[J]. Expert Opinion on Drug Safety, 2017. 3. Danek P J, Wójcikowski J, Daniel W A. Asenapine and iloperidone decrease the expression of major cytochrome P450 enzymes CYP1A2 and CYP3A4 in human hepatocytes. A significance for drug-drug interactions during combined therapy[J]. Toxicology and Applied Pharmacology. 2020, 406: 115239.

TargetMol Library Books文献引用

1. Danek P J, Wójcikowski J, Daniel W A. Asenapine and iloperidone decrease the expression of major cytochrome P450 enzymes CYP1A2 and CYP3A4 in human hepatocytes. A significance for drug-drug interactions during combined therapy. Toxicology and Applied Pharmacology. 2020, 406: 115239 2. Danek P J, Daniel W A.The Novel Atypical Antipsychotic Lurasidone Affects Cytochrome P450 Expression in the Liver and Peripheral Blood Lymphocytes.International Journal of Molecular Sciences.2023, 24(23): 16796.
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相关化合物库

该产品包含在如下化合物库中:
Dopamine Receptor inhibitor kit

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母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

Lurasidone 367514-87-2 GPCR/G Protein Neuroscience 5-HT Receptor Dopamine Receptor SM 13496 SM-13496 SM13496 鲁拉西酮 inhibit Serotonin Receptor 5-hydroxytryptamine Receptor Inhibitor inhibitor

 

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