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Submit ReviewTHIQ is a potent and selective melanocortin 4 (MC4) receptor agonist (IC50 values are 1.2, 761 and 2067 nM for human MC4, MC3 and MC1 receptors respectively). Enhances intracavernosal pressure and stimulates erectile activity in rats ex copula following systemic administration.
分子量 | 589.17 |
公式 | C33H41ClN6O2 |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 312637-48-2 |
PubChem ID | 9938402 |
InChI Key | HLCHESOMJVGDSJ-LOYHVIPDSA-N |
Smiles | O=[C@@]([C@H](NC([C@H]5CC(C=CC=C6)=C6CN5)=O)CC4=CC=C(Cl)C=C4)N1CCC(CN2N=CN=C2)(C3CCCCC3)CC1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 5.89 | 10 |
以下数据基于产品分子量 589.17。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.1 mM | 16.97 mL | 84.87 mL | 169.73 mL |
0.5 mM | 3.39 mL | 16.97 mL | 33.95 mL |
1 mM | 1.7 mL | 8.49 mL | 16.97 mL |
5 mM | 0.34 mL | 1.7 mL | 3.39 mL |
参考文献是支持产品生物活性的出版物。
Sebhat et al (2002) Design and pharmacology of N-[(3R)-1,2,3,4-Tetrahydroisoquinolinium-3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-methyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective melanocorti J.Med.Chem. 45 4589 PMID: 12361385
Martin et al (2002) Activation of melanocortin MC4 receptors increases erectile activity in rats ex copula. Eur.J.Pharmacol. 454 71 PMID: 12409007
Mutulis et al (2004) New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of "THIQ". J.Med.Chem. 47 4613 PMID: 15317471
If you know of a relevant reference for THIQ, please let us know.
关键词: THIQ, THIQ supplier, Potent, selective, MC4R, receptors, agonists, Melanocortin, Receptors, 3032, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 THIQ 的部分引用包括:
Garfield et al (2015) A neural basis for melanocortin-4 receptor-regulated appetite. Nat Neurosci 18 863 PMID: 25915476
Sohn et al (2013) Melanocortin 4 receptors reciprocally regulate sympathetic and parasympathetic preganglionic neurons. Int J Biol Sci 152 612 PMID: 23374353
Huang and Tao (2014) A small molecule agonist THIQ as a novel pharmacoperone for intracellularly retained melanocortin-4 receptor mutants. Front Pharmacol 10 817 PMID: 25076858
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Recently, we demonstrated that the deletion of the NFKB1 gene, which encodes the p50 NF-kappa B subunit, causes impairment in social behaviours, with reductions in social interactions in mice. In this work, we tested the acute effects of THIQ, a selective melanocortin 4 receptor (MC4R) agonist. THIQ treatment increased social interactions both in wild type and p50-/- mice. In particular, after treatment with THIQ, p50-/- mice showed a prosocial behaviour analogous to that of basal WT mice.
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.