Lurasidone (SM-13496)
(Synonyms: 鲁拉西酮; SM-13496) 目录号 : GC30926
An atypical antipsychotic
Cas No.:367514-87-2
Sample solution is provided at 25 µL, 10mM.
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Lurasidone is an atypical antipsychotic that binds to dopamine D2, serotonin (5-HT) receptor subtypes 5-HT2A, 5-HT1A, and 5-HT7, and α2C-adrenergic receptors (Kis = 1.68, 2.03, 6.75, 0.495, and 10.8 nM, respectively).1 In vivo, pre-training administration of lurasidone (1 and 3 mg/kg) reverses impairment in step-through latency and passive avoidance in a foot shock test induced by MK-801 in rats. It reverses MK-801-induced learning impairment in the Morris water maze as well as reference and working memory impairment in the radial arm maze in rats.2 Lurasidone also decreases immobility in the tail suspension and forced swim tests, indicating antidepressant-like activity in mice.3 Formulations containing lurasidone have been used in the treatment of schizophrenia and mood disorders.
1.Ishiyama, T., Tokuda, K., Ishibashi, T., et al.Lurasidone (SM-13496), a novel atypical antipsychotic drug, reverses MK-801-induced impairment of learning and memory in the rat passive-avoidance testEur. J. Pharmacol.572(2-3)160-170(2007) 2.Enomoto, T., Ishibashi, T., Tokuda, K., et al.Lurasidone reverses MK-801-induced impairment of learning and memory in the Morris water maze and radial-arm maze tests in ratsBehav. Brain Res.186(2)197-207(2008) 3.Cates, L.N., Roberts, A.J., Huitron-Resendiz, S., et al.Effects of lurasidone in behavioral models of depression. Role of the 5-HT7 receptor subtypeNeuropharmacology70211-217(2013)
Animal experiment: | SD rats are individually isolated in clear plastic cages and injected with methamphetamine (MAP) (1 mg/kg i.p.) 1 h after the administration of drugs or vehicle. In the test of persistence of the effect, Lurasidone (SM-13496) is administered 1, 2, 4, and 8 h before the MAP injection. Locomotor activity is measured for 80 min from 10 min after MAP injection. Four or five groups of 6 to 13 rats are used to calculate the ED50 value that inhibits MAP-induced hyperactivity by 50% of the animals tested[1]. |
References: [1]. Ishibashi T, et al. Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity. J Pharmacol Exp Ther. 2010 Jul;334(1):171-81. | |
| Cas No. | 367514-87-2 | SDF | |
| 别名 | 鲁拉西酮; SM-13496 | ||
| Canonical SMILES | O=C([C@H]1[C@H]2C[C@H](CC2)[C@@H]31)N(C[C@H](CCCC4)[C@@H]4CN5CCN(CC5)C6=NSC7=CC=CC=C67)C3=O | ||
| 分子式 | C28H36N4O2S | 分子量 | 492.68 |
| 溶解度 | DMSO : 20.83 mg/mL (42.28 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0297 mL | 10.1486 mL | 20.2972 mL |
| 5 mM | 0.4059 mL | 2.0297 mL | 4.0594 mL |
| 10 mM | 0.203 mL | 1.0149 mL | 2.0297 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet