Lumateperone tosylate ITI-007 tosylate|cas:1187020-80-9|西域试剂

Lumateperone tosylate ITI-007 tosylate,99.42%

产品编号：Bellancom-19733| CAS NO：1187020-80-9| 分子式：C₃₁H₃₆FN₃O₄S| 分子量：565.70

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-19733	￥600.00	杭州北京（现货）
Bellancom-19733	￥1000.00	杭州北京（现货）
Bellancom-19733	￥2000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Lumateperone tosylate ITI-007 tosylate

产品介绍

Lumateperone (ITI-007) tosylate 是一种 5-HT2A 受体拮抗剂 (Ki = 0.54 nM)、突触前 D2 受体的部分激动剂和突触后 D2 受体的拮抗剂 (Ki = 32 nM)、多巴胺 D1 受体调节剂。Lumateperone tosylate 具有抗癌活性, 可用于精神分裂症等相关精神病的研究。

生物活性

Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.

体外研究

Lumateperone (2-30 μM) tosylate has anti-tumor activity and can inhibit cell proliferation in a dose-dependent manner.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	RPMI-8226 cells
Concentration:	2-30 μM
Incubation Time:
Result:	Inhibited cell growth with the IC₅₀ value of 17.30 μM.

体内研究
(In Vivo)

Lumateperone (i.p., 1-10 mg/kg) tosylate promotes NMDA and AMPA-induced currents in a dopamine D 1 receptor-dependent manner and increases the release of dopamine and glutamate in rat mPFC slices.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult male Sprague-Dawley rats
Dosage:	1-10 mg/kg
Administration:	Intraperitoneal injection
Result:	Inhibited avoidance response at concentrations of 1, 3 and 10 mg/kg after 20 minutes. Promoted NMDA and AMPA-sensitive currents, also significantly increased dopamine and glutamate release at 10 mg/kg in mPFC cone cells of rat.

体内研究

Lumateperone (i.p., 1-10 mg/kg) tosylate promotes NMDA and AMPA-induced currents in a dopamine D 1 receptor-dependent manner and increases the release of dopamine and glutamate in rat mPFC slices.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult male Sprague-Dawley rats
Dosage:	1-10 mg/kg
Administration:	Intraperitoneal injection
Result:	Inhibited avoidance response at concentrations of 1, 3 and 10 mg/kg after 20 minutes. Promoted NMDA and AMPA-sensitive currents, also significantly increased dopamine and glutamate release at 10 mg/kg in mPFC cone cells of rat.

体内研究

Lumateperone (i.p., 1-10 mg/kg) tosylate promotes NMDA and AMPA-induced currents in a dopamine D 1 receptor-dependent manner and increases the release of dopamine and glutamate in rat mPFC slices.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult male Sprague-Dawley rats
Dosage:	1-10 mg/kg
Administration:	Intraperitoneal injection
Result:	Inhibited avoidance response at concentrations of 1, 3 and 10 mg/kg after 20 minutes. Promoted NMDA and AMPA-sensitive currents, also significantly increased dopamine and glutamate release at 10 mg/kg in mPFC cone cells of rat.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (176.77 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 80°C) (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7677 mL	8.8386 mL	17.6772 mL
5 mM	0.3535 mL	1.7677 mL	3.5354 mL
10 mM	0.1768 mL	0.8839 mL	1.7677 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

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: ≥ 2.5 mg/mL (4.42 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.42 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.42 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.42 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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。
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