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Submit ReviewJKC 363 is a potent and selective melanocortin MC4 receptor antagonist (IC50 values are 0.5 and 44.9 nM at MC4 and MC3 respectively) that antagonizes the effects of α-MSH. Suppresses thyrotropin-releasing hormone (TRH) release, attenuates food intake and reduces formalin-induced pain in vivo.
分子量 | 1506.72 |
公式 | C69H91N19O16S2 |
序列 |
XEHXRWGCPPKD (Modifications: Disulfide bridge between 1 - 8, X-1 = Mpr, X-4 = D-2-Nal, Asp-12 = C-terminal amide) |
储存 | Store at -20°C |
CAS Number | 436083-30-6 |
PubChem ID | 90488844 |
InChI Key | DBHQKXPXPFYXHK-DUOXTXSESA-N |
Smiles | NCCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC2=CNC=N2)C(=O)N[C@H](CC2=CC3=CC=CC=C3C=C2)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC2=CNC3=C2C=CC=C3)C(=O)NCC(=O)N1)C(=O)N[C@@H](CC(O)=O)C(N)=O |
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.
参考文献是支持产品生物活性的出版物。
Kim et al (2002) Effects of melanocortin receptor ligands on thyrotropin-releasing hormone release: evidence for the differential roles of melanocortin 3 and 4 receptors. J.Neuroendocrinol. 14 276 PMID: 11963824
Bellasio et al (2003) Melanocortin receptor agonists and antagonists modulate nociceptive sensitivity in the mouse formalin test. Eur.J.Pharmacol. 482 127 PMID: 14660013
Verty et al (2004) Evidence for an interaction between CB1 cannabinoid and melanocortin MCR-4 receptors in regulating food intake. Endocrinology 145 3224 PMID: 15033920
关键词: JKC 363, JKC 363 supplier, Potent, selective, MC4R, receptor, antagonists, Receptors, Melanocortin, JKC363, 3426, Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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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.