Lumateperone tosylate|1187020-80-9|(ITI-007 tosylate)-陌孚医药/Medlife

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Lumateperone tosylate (Synonyms: ITI-007 tosylate)

目录号: PL04932 纯度: ≥99%

CAS No. :1187020-80-9

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中文名称	Lumateperone tosylate
中文别名	1-(4-氟苯基)-4-[(6bR,10aS)-2,3,6b,9,10,10a-六氢-3-甲基-1H-吡啶并[3',4':4,5]吡咯并[1,2,3-de]喹喔啉-8(7H)-基]-1-丁酮对甲苯磺酸盐;lumateperone (Tosylate);lumateperone (Tosylate)卢美哌隆对甲苯磺酸盐
英文名称	Lumateperone tosylate
英文别名	lumateperone (Tosylate);ITI-007;ITI 007;Lumateperone(ITI-007);lumateperone Tosylate;JIE88N006O;Lumateperone tosylate (USAN);Lumateperone tosylate [USAN];ITI007;Caplyta (TN);D11170;Q27281520
Cas No.	1187020-80-9
分子式	C₃₁H₃₆FN₃O₄S
分子量	565.70
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

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.

性状

Solid

IC50 & Target[1][2]

5-HT2A Receptor 0.54 nM (Ki)

体外研究(In Vitro)

Lumateperone (2-30 μM) tosylate has anti-tumor activity and can inhibit cell proliferation in a dose-dependent manner.
has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay

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.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Jinyuan Zhang, et al. Identification of Trovafloxacin, Ozanimod, and Ozenoxacin as Potent c-Myc G-quadruplex Stabilizers to Suppress c-Myc Transcription and Myeloma Growth. Mol Inform. 2022 Mar 30:e2200011.
[2]. J Titulaer, et al. Lumateperone-mediated effects on prefrontal glutamatergic receptor-mediated neurotransmission: A dopamine D1 receptor dependent mechanism. Eur Neuropsychopharmacol. 2022 Jul 22;62:22-35.

溶解度数据	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

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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