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Lurasidone hydrochloride

Lurasidone hydrochloride

产品编号 T1735   CAS 367514-88-3
别名: Lurasidone HCl, SM-13496 (Hydrochloride), 盐酸鲁拉西酮, SM-13496

Lurasidone hydrochloride (Lurasidone HCl) 是多巴胺 D2和5-HT7的拮抗剂,IC50值分别为 1.68 和 0.495 nM,用于治疗精神分裂症和双相情感障碍。它也是5-HT1A 受体的部分激动剂,IC50值为 6.75 nM。

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Lurasidone hydrochloride Chemical Structure
Lurasidone hydrochloride, CAS 367514-88-3
规格 价格/CNY 货期 数量
5 mg ¥ 198 现货
10 mg ¥ 327 现货
25 mg ¥ 565 现货
50 mg ¥ 913 现货
100 mg ¥ 1,490 现货
200 mg ¥ 2,390 现货
500 mg ¥ 3,970 现货
1 mL * 10 mM (in DMSO) ¥ 291 现货
其他形式的 Lurasidone hydrochloride:
产品目录号及名称: Lurasidone hydrochloride (T1735)
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生物活性
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存储 & 溶解度
参考文献
产品描述 Lurasidone hydrochloride (Lurasidone HCl) is a thiazole derivative and atypical antipsychotic agent that functions as a dopamine D2 receptor antagonist; serotonin 5-HT2 receptor antagonist, serotonin 5-HT7 receptor antagonist, an antagonist of the adrenergic α2A and α2C receptors, as well as a partial serotonin 5-HT1A receptor agonist. It is used in the treatment of schizophrenia and bipolar disorder.
靶点活性 5-HT1A:6.75 nM, D2 receptor:1.68 nM, Noradrenaline α2C:10.8 nM, 5-HT2A:2.03 nM, 5-HT7:0.495 nM
体外活性 Lurasidone antagonizes dopamine-stimulated [35S]GTPγS binding at human dopamine D2L receptor in a concentration-dependent manner with a KB value of 2.8 nM. Lurasidone antagonizes 5-HT-stimulated cAMP accumulation in the CHO/h5-HT7 cells with a KB value of 2.6 nM. Lurasidone partially stimulates [35S]GTPγS binding to the membrane preparation for human 5-HT1A receptors with a maximum effect of 33%. Lurasidone dose-dependently increases the ratio of DOPAC/dopamine in rat frontal cortex and striatum. [1]
体内活性 The inhibitory actions of Lurasidone on MAP-induced hyperactivity persists for more than 8 hours, and the ED50 values of the action at 1 hour, 2 hours, 4 hours, and 8 hours after the treatment are 2.3 mg/kg, 0.87 mg/kg, 1.6 mg/kg, and 5.0 mg/kg, respectively. Lurasidone (1 mg/kg–10 mg/kg) dose-dependently inhibits conditioned avoidance response in rats with ED50 of 6.3 mg/kg. Lurasidone dose-dependently inhibits TRY-induced forepaw clonic seizure and p-CAMP-induced hyperthermia in rats with ED50 of 5.6 mg/kg and 3.0 mg/kg, respectively. Lurasidone (0.3 mg/kg–30 mg/kg) dose-dependently and significantly increases the number of shocks received by rats in the Vogel's conflict test with MED of 10 mg/kg. Lurasidone (3 mg/kg, 2 weeks) significantly suppresses hyperactivity behavior in olfactory bulbectomy model rats. Lurasidone (700 mg/kg–1000 mg/kg) slightly prolongs the duration of loss of righting reflexes elicited by hexobarbital (anesthesia) in mice in a dose-dependent manner. [1] Lurasidone (30 mg/kg, p.o.) significantly and dose-dependently reverses the MK-801-induced impairment of the passive-avoidance response of rats. [2] Lurasidone (3 mg/kg p.o.) potently reverses MK-801-induced learning impairment in the Morris water maze test in rats. Lurasidone (3 mg/kg p.o.) potently reverses MK-801-induced reference memory impairment and moderately but not significantly attenuates MK-801-induced working memory impairment in the radial-arm maze test. [3] Lurasidone (10 mg/kg) treatment increases total BDNF mRNA levels in rat prefrontal cortex and, to less extent, in hippocampus. Lurasidone (10 mg/kg) significantly increases the levels of mature BDNF protein in rat prefrontal cortex, without affect the protein levels of the neurotrophin (both precursor and mature forms) in hippocampal extracts. [4]
别名 Lurasidone HCl, SM-13496 (Hydrochloride), 盐酸鲁拉西酮, SM-13496
分子量 529.14
分子式 C28H36N4O2S·HCl
CAS No. 367514-88-3

存储

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

溶解度

DMSO: 5.29 mg/mL (10 mM), Sonification 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 1.8899 mL 9.4493 mL 18.8986 mL 47.2465 mL
5 mM 0.378 mL 1.8899 mL 3.7797 mL 9.4493 mL
10 mM 0.189 mL 0.9449 mL 1.8899 mL 4.7246 mL

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参考文献

1. Ishibashi T, et al. J Pharmacol Exp Ther, 2010, 334(1), 171-181. 2. Ishiyama T, et al. Eur J Pharmacol, 2007, 572(2-3), 160-170. 3. Enomoto T, et al. Behav Brain Res, 2008, 186(2), 197-207. 4. Fumagalli F, et al. Int J Neuropsychopharmacol, 2012, 15(2), 235-246. 5. Danek P J, Wójcikowski J, Daniel W A. The atypical neuroleptics iloperidone and lurasidone inhibit human cytochrome P450 enzymes in vitro. Evaluation of potential metabolic interactions[J]. Pharmacological reports: PR. 2020, 72(6): 1685-1694. 6. Marta Kot, Anna Haduch, Mariusz Papp, Władysława A. Daniel. The effect of chronic treatment with lurasidone on rat liver cytochrome P450 expression and activity in the chronic mild stress (CMS) model of depression [J]. Drug Metabolism and Disposition. 2017, 45(12): 1336-1344.

文献引用

1. Danek P J, Daniel W A. The Atypical Antipsychotic Lurasidone Affects Brain but Not Liver Cytochrome P450 2D (CYP2D) Activity. A Comparison with Other Novel Neuroleptics and Significance for Drug Treatment of Schizophrenia. Cells. 2022, 11(21): 3513. 2. Kot M, Haduch A, Papp M, et al. The effect of chronic treatment with lurasidone on rat liver cytochrome P450 expression and activity in the chronic mild stress (CMS) model of depression. Drug Metabolism and Disposition. 2017, 45(12): 1336-1344 3. Danek P J, Wójcikowski J, Daniel W A. The atypical neuroleptics iloperidone and lurasidone inhibit human cytochrome P450 enzymes in vitro. Evaluation of potential metabolic interactions. Pharmacological Reports:PR. 2020, 72(6): 1685-1694
2'-O-Methylisoliquiritigenin UCSF924 Bromocriptine mesylate Mesoridazine Besylate Promazine hydrochloride L-DOPA Blonanserin 9-FLUORENOL

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌临床化合物库 神经退行性疾病化合物库 抗癌上市药物库 血管生成库 已知活性化合物库 肝脏毒性化合物库 抗COVID-19化合物库 上市药物库 FDA 上市药物库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

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 hydrochloride 367514-88-3 GPCR/G Protein Neuroscience Dopamine Receptor 5-HT Receptor Norepinephrine Lurasidone HCl Inhibitor 5-hydroxytryptamine Receptor SM-13496 (Hydrochloride) Lurasidone Lurasidone Hydrochloride SM 13496 inhibit 盐酸鲁拉西酮 SM-13496 Serotonin Receptor SM13496 inhibitor

 

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