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Submit ReviewHS 024 is a highly potent melanocortin MC4 receptor antagonist (Ki values are 0.29, 18.6, 5.45 and 3.29 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake, and blocks α-MSH- and MTII-induced hypotension and bradycardia in rats, following central administration in vivo.
分子量 | 1266.5 |
公式 | C58H79N19O10S2 |
序列 |
CXRHXRWGC (Modifications: Cys-1 = N-terminal Ac, X-2 = Nle, X-5 = Nal, Cys-9 = C-terminal amide, Disulfide bridge: 1-9) |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 212370-59-7 |
PubChem ID | 25081552 |
InChI Key | PUOCNCOPVAOMDE-LQXMKOPKSA-N |
Smiles | CCCC[C@@H]1NC(=O)[C@H](CSSC[C@H](NC(=O)CNC(=O)[C@H](CC2=CNC3=C2C=CC=C3)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](CC2=CC3=CC=CC=C3C=C2)NC(=O)[C@H](CC2=CNC=N2)NC(=O)[C@H](CCCNC(N)=N)NC1=O)C(N)=O)NC(C)=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.
溶解性 | Soluble to 0.50 mg/ml in water |
参考文献是支持产品生物活性的出版物。
Jonsson et al (2001) Melanocortin receptor agonist transiently increases oxygen consumption in rats. Neuroreport 12 3703 PMID: 11726778
Jonsson et al (2002) Food conversion is transiently affected during 4-week chronic administration of melanocortin agonist and antagonist in rats. J.Endocrinol. 173 517 PMID: 12065241
Kask et al (1998) Discovery of a novel superpotent and selective melanocortin-4 receptor antagonist (HS024): evaluation in vitro and in vivo. Endocrinology 139 5006 PMID: 9832440
If you know of a relevant reference for HS 024, please let us know.
关键词: HS 024, HS 024 supplier, potent, MC4R, receptor, antagonists, Receptors, Melanocortin, HS024, 1832, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 HS 024 的部分引用包括:
Simamura et al (2015) Melanocortins contribute to sequential differentiation and enucleation of human erythroblasts via melanocortin receptors 1, 2 and 5. J Neurochem 10 e0123232 PMID: 25860801
Nepomuceno et al (2018) Re-evaluation of Adrenocorticotropic Hormone and Melanocyte Stimulating Hormone Activation of GPR139 in Vitro. Front Pharmacol 9 157 PMID: 29599718
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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.