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Lurasidone hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Lurasidone hydrochloride图片
CAS NO:367514-88-3
包装与价格:
包装价格(元)
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议
1 g电议
5 g电议

产品名称
盐酸鲁拉西酮
SM-13496 Hydrochloride
产品介绍
Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) 是dopamine D25-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。
生物活性

Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of bothdopamine D2and5-HT7withIC50s of 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of5-HT1Areceptor with anIC50of 6.75 nM.

IC50& Target

5-HT7Receptor

0.495 nM (IC50)

5-HT1AReceptor

6.75 nM (IC50)

D2Receptor

1.68 nM (IC50)

体外研究
(In Vitro)

Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of dopamine D2and 5-HT7with 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-HT1Areceptor with an IC50of 6.75±0.97 nM.In vitroreceptor binding experiments reveal that Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) demonstrates affinity for dopamine D2and 5-HT2Areceptors higher than other tested antipsychotics. Lurasidone does not increase [35S]GTPγS binding to the membrane preparations for dopamine D2receptors by itself, but it antagonizes dopamine-stimulated [35S]GTPγS binding in a concentration-dependent manner with a KBvalue of 2.8±1.1 nM[1].

体内研究
(In Vivo)

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)) (ED50values 2.3 to 5.0 mg/kg) shows a comparable potency with olanzapine (ED50values 1.1 to 5.1 mg/kg), higher potency than clozapine (ED509.5 to 290 mg/kg), and slightly lower potency than haloperidol (ED50values 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 ED50values are 6.3 mg/kg. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) dose-dependently inhibits TRY-induced forepaw clonic seizure and p-CAMP-induced hyperthermia with ED50values 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)[1].

Clinical Trial
分子量

529.14

性状

Solid

Formula

C28H37ClN4O2S

CAS 号

367514-88-3

中文名称

盐酸鲁拉西酮

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

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)

H2O :< 0.1 mg/mL(insoluble)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.8899 mL9.4493 mL18.8986 mL
5 mM0.3780 mL1.8899 mL3.7797 mL
10 mM0.1890 mL0.9449 mL1.8899 mL
*

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

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
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在本网站选购。