Talnetant | SB 223412 | NK3 Receptor Antagonist | AmBeed-信号通路专用抑制剂

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Talnetant {[allProObj[0].p_purity_real_show]}

货号：A303351 同义名： SB 223412

Talnetant is a potent and selective NK3 receptor antagonist (ki=1.4 nM, hNK-3-CHO), and is 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 μM.

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Talnetant 化学结构
CAS号：174636-32-9

Talnetant 3D分子结构
CAS号：174636-32-9

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Talnetant 纯度/质量文件产品仅供科研

货号：A303351 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nature, 2025. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 更多 >

Talnetant 生物活性

描述

Neurokinin-3 (NK-3) is a seven-transmembrane G protein that mediates the pharmacological actions of tachykinins. Talnetant is a selective, non-peptide antagonist of NK-3 receptor that displays high binding affinity to cloned hNK-3 receptors expressed in CHO cells with a K_i value of 1.4±0.2nM. Talnetant inhibited neurokinin B (1nM)-induced Ca²⁺ mobilization in hNK-3-HEK 293 cells with an IC50 value of 16.6±1.6nM. Following 6-h intravenous infusion at 1mg/kg/h, the brain tissue concentration of Talnetant in rats was 356ng/g and the ratio of brain tissue/plasma concentration was approximately 0.20. The oral administration of Talnetant in mice resulted in a dose-dependent inhibition of senktide (1mg/kg)-induced behavioral effects with an ED50 value of 12.2mg/kg. The pretreatment of Talnetant (0.5-2 mg/kg, i.v.) also led to a dose-related inhibition of senktide (25μg, i.v.)-induced miosis in rabbits with an ED50 value of 0.44mg/kg^[3].

Talnetant 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00049946	Schizophrenia	Phase 2	Completed	-	-
NCT00300963	Schizophrenia	Phase 2	Completed	-	United States, Arkansas ... 展开 >> GSK Investigational Site Little Rock, Arkansas, United States, 72201 United States, California GSK Investigational Site Anaheim, California, United States, 92805 GSK Investigational Site Cerritos, California, United States, 90703 GSK Investigational Site Garden Grove, California, United States, 92845 GSK Investigational Site Glendale, California, United States, 91206 GSK Investigational Site National City, California, United States, 91950 GSK Investigational Site Oceanside, California, United States, 92056 GSK Investigational Site Pico Rivera, California, United States, 90660 GSK Investigational Site Rosemead, California, United States, 91770 GSK Investigational Site San Diego, California, United States, 92123 GSK Investigational Site Upland, California, United States, 91786 United States, District of Columbia GSK Investigational Site Washington, District of Columbia, United States, 20016 United States, Florida GSK Investigational Site North Miami, Florida, United States, 33161 United States, Georgia GSK Investigational Site Atlanta, Georgia, United States, 30308 United States, Missouri GSK Investigational Site St. Louis, Missouri, United States, 63118 United States, New Jersey GSK Investigational Site Clementon, New Jersey, United States, 08021 United States, Pennsylvania GSK Investigational Site Philadelphia, Pennsylvania, United States, 19131 United States, Texas GSK Investigational Site Austin, Texas, United States, 78756 GSK Investigational Site Irving, Texas, United States, 75062 United States, Virginia GSK Investigational Site Richmond, Virginia, United States, 23294 收起 <<
NCT00103727	Schizophrenia	Phase 2	Completed	-	United States, Arkansas ... 展开 >> GSK Investigational Site Little Rock, Arkansas, United States, 72201 United States, California GSK Investigational Site Anaheim, California, United States, 92805 GSK Investigational Site Cerritos, California, United States, 90703 GSK Investigational Site Garden Grove, California, United States, 92845 GSK Investigational Site Glendale, California, United States, 91206 GSK Investigational Site National City, California, United States, 91950 GSK Investigational Site Oceanside, California, United States, 92056 GSK Investigational Site Pico Rivera, California, United States, 90660 GSK Investigational Site Rosemead, California, United States, 91770 GSK Investigational Site San Diego, California, United States, 92123 GSK Investigational Site San Diego, California, United States, 92126 GSK Investigational Site Upland, California, United States, 91786 United States, District of Columbia GSK Investigational Site Washington, District of Columbia, United States, 20016 United States, Florida GSK Investigational Site North Miami, Florida, United States, 33161 United States, Georgia GSK Investigational Site Atlanta, Georgia, United States, 30308 United States, Illinois GSK Investigational Site Oak Brook, Illinois, United States, 60523 United States, Missouri GSK Investigational Site St. Louis, Missouri, United States, 63118 United States, New Jersey GSK Investigational Site Clementon, New Jersey, United States, 08021 United States, Pennsylvania GSK Investigational Site Philadelphia, Pennsylvania, United States, 19131 United States, Texas GSK Investigational Site Austin, Texas, United States, 78756 GSK Investigational Site Irving, Texas, United States, 75062 United States, Virginia GSK Investigational Site Richmond, Virginia, United States, 23294 收起 <<

Talnetant 参考文献

[1]Liem-Moolenaar M, Gray FA, et al. Psychomotor and cognitive effects of a single oral dose of talnetant (SB223412) in healthy volunteers compared with placebo or haloperidol. J Psychopharmacol. 2010 Jan;24(1):73-82.

[2]Dawson LA, Cato KJ, et al. In vitro and in vivo characterization of the non-peptide NK3 receptor antagonist SB-223412 (talnetant): potential therapeutic utility in the treatment of schizophrenia. Neuropsychopharmacology. 2008 Jun;33(7):1642-52.

[3]Giardina, G. A., Raveglia, L. F. et al. Discovery of a novel xlass of selective non-peptide antagonists for the human neuronkinin-2 receptor. 2. Identification of (S)-N-(1-phenylpropyl)-3-hydroxy-2-phenylquinoline-4-carboxamide (SB223412). J Med Chem. 1999. 42(6):1053-65.

Talnetant 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.07mL

2.61mL

1.31mL

26.15mL

5.23mL

2.61mL

Talnetant 技术信息

CAS号	174636-32-9
分子式	C₂₅H₂₂N₂O₂
分子量	382.45
SMILES Code	O=C(C1=C(O)C(C2=CC=CC=C2)=NC3=CC=CC=C13)N[C@H](C4=CC=CC=C4)CC
MDL No.	MFCD00944075

别名	SB 223412
运输	蓝冰
InChI Key	BIAVGWDGIJKWRM-FQEVSTJZSA-N
Pubchem ID	5311424

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

细胞实验：

DMSO: 105 mg/mL(274.54 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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

方案一

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00049946	Schizophrenia	Phase 2	Completed	-	-
NCT00300963	Schizophrenia	Phase 2	Completed	-	United States, Arkansas ... 展开 >> GSK Investigational Site Little Rock, Arkansas, United States, 72201 United States, California GSK Investigational Site Anaheim, California, United States, 92805 GSK Investigational Site Cerritos, California, United States, 90703 GSK Investigational Site Garden Grove, California, United States, 92845 GSK Investigational Site Glendale, California, United States, 91206 GSK Investigational Site National City, California, United States, 91950 GSK Investigational Site Oceanside, California, United States, 92056 GSK Investigational Site Pico Rivera, California, United States, 90660 GSK Investigational Site Rosemead, California, United States, 91770 GSK Investigational Site San Diego, California, United States, 92123 GSK Investigational Site Upland, California, United States, 91786 United States, District of Columbia GSK Investigational Site Washington, District of Columbia, United States, 20016 United States, Florida GSK Investigational Site North Miami, Florida, United States, 33161 United States, Georgia GSK Investigational Site Atlanta, Georgia, United States, 30308 United States, Missouri GSK Investigational Site St. Louis, Missouri, United States, 63118 United States, New Jersey GSK Investigational Site Clementon, New Jersey, United States, 08021 United States, Pennsylvania GSK Investigational Site Philadelphia, Pennsylvania, United States, 19131 United States, Texas GSK Investigational Site Austin, Texas, United States, 78756 GSK Investigational Site Irving, Texas, United States, 75062 United States, Virginia GSK Investigational Site Richmond, Virginia, United States, 23294 收起 <<
NCT00103727	Schizophrenia	Phase 2	Completed	-	United States, Arkansas ... 展开 >> GSK Investigational Site Little Rock, Arkansas, United States, 72201 United States, California GSK Investigational Site Anaheim, California, United States, 92805 GSK Investigational Site Cerritos, California, United States, 90703 GSK Investigational Site Garden Grove, California, United States, 92845 GSK Investigational Site Glendale, California, United States, 91206 GSK Investigational Site National City, California, United States, 91950 GSK Investigational Site Oceanside, California, United States, 92056 GSK Investigational Site Pico Rivera, California, United States, 90660 GSK Investigational Site Rosemead, California, United States, 91770 GSK Investigational Site San Diego, California, United States, 92123 GSK Investigational Site San Diego, California, United States, 92126 GSK Investigational Site Upland, California, United States, 91786 United States, District of Columbia GSK Investigational Site Washington, District of Columbia, United States, 20016 United States, Florida GSK Investigational Site North Miami, Florida, United States, 33161 United States, Georgia GSK Investigational Site Atlanta, Georgia, United States, 30308 United States, Illinois GSK Investigational Site Oak Brook, Illinois, United States, 60523 United States, Missouri GSK Investigational Site St. Louis, Missouri, United States, 63118 United States, New Jersey GSK Investigational Site Clementon, New Jersey, United States, 08021 United States, Pennsylvania GSK Investigational Site Philadelphia, Pennsylvania, United States, 19131 United States, Texas GSK Investigational Site Austin, Texas, United States, 78756 GSK Investigational Site Irving, Texas, United States, 75062 United States, Virginia GSK Investigational Site Richmond, Virginia, United States, 23294 收起 <<
NCT00101985	Irritable Colon	Phase 2	Completed	-	-

Talnetant {[allProObj[0].p_purity_real_show]}

Talnetant 纯度/质量文件产品仅供科研

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Talnetant 质控信息

Talnetant 生物活性

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Talnetant 实验方案

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Talnetant {[allProObj[0].p_purity_real_show]}

Talnetant 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Talnetant 质控信息

Talnetant 生物活性

Talnetant 临床研究

Talnetant 参考文献

Talnetant 实验方案

Talnetant 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Talnetant 纯度/质量文件产品仅供科研