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Submit ReviewSHU 9119
说明： MC3 and MC4 antagonist; MC5 partial agonist
纯度： ≥95% (HPLC)
生物活性 for SHU 9119
SHU 9119 is a potent melanocortin MC3 and MC4 receptor antagonist (IC50 values are 0.23 and 0.06 nM respectively) and MC5 partial agonist (EC50 = 0.12 nM). Upregulates expression of genes promoting lipogenesis and triglyceride storage (SCD1, LPL, ACCα and FAS), increases triglyceride synthesis and promotes insulin resistance. Increases food intake, body weight and fat mass when administered centrally in vivo.
技术数据 for SHU 9119
| 分子量 | 1074.25 |
| 公式 | C54H71N15O9 |
| 序列 |
XDHXRWK (Modifications: X-1 = Ac-Nle, X-4 = D-2-Nal, Lys-7 = C-terminal amide, cyclized Asp-2 - Lys-7) |
| 储存 | Store at -20°C |
| 纯度 | ≥95% (HPLC) |
| CAS Number | 168482-23-3 |
| PubChem ID | 9898183 |
| InChI Key | GGYWLZFXFKFWKL-XOJVSUSESA-N |
| Smiles | CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=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)NC1=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.
溶解性数据 for SHU 9119
| 溶解性 | Soluble to 0.20 mg/ml in water |
产品说明书 for SHU 9119
参考文献 for SHU 9119
参考文献是支持产品生物活性的出版物。
Hruby et al (1995) Cyclic lactam α-melanotropin analogues of Ac-Nle4-cyclo[Asp5,D-Phe7,Lys10] a-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency a J.Med.Chem. 38 3454 PMID: 7658432
Grieco et al (2007) Further structure-activity studies with lactam derivatives of MT-II and SHU-9119: Their activity and selectivity at human melanocortin receptors 3, 4 and 5. Peptides 28 1191 PMID: 17482720
Nogueiras et al (2007) The central melanocortin system directly controls peripheral lipid metabolism. J.Clin.Invest. 117 3475 PMID: 17885689
If you know of a relevant reference for SHU 9119, please let us know.
关键词: SHU 9119, SHU 9119 supplier, MC3R, MC4R, antagonists, MC5R, partial, agonists, Receptors, Melanocortin, SHU9119, 3420, Tocris Bioscience
7 篇 SHU 9119 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SHU 9119 的部分引用包括：
Ewa et al (2021) Novel bifunctional hybrid compounds designed to enhance the effects of opioids and antagonize the pronociceptive effects of nonopioid peptides as potent analgesics in a rat model of neuropathic pain. Pain 162 432-445 PMID: 32826750
Gerhard et al (2014) The use of amphipols for NMR structural characterization of 7-TM proteins. J Membr Biol 247 957-64 PMID: 24858950
Ronald N et al (2020) Lipid-gated monovalent ion fluxes regulate endocytic traffic and support immune surveillance. Science 367 301-305 PMID: 31806695
Päärn et al (2020) The constitutive activity of melanocortin-4 receptors in cAMP pathway is allosterically modulated by zinc and copper ions. J Neurochem 153 346-361 PMID: 31792980
Alhadeff et al (2018) A Neural Circuit for the Suppression of Pain by a Competing Need State. Cell 173 140 PMID: 29570993
Tao and Huang (2014) Ipsen 5i is a Novel Potent Pharmacoperone for Intracellularly Retained Melanocortin-4 Receptor Mutants. Front Endocrinol (Lausanne) 5 131 PMID: 25136332
Jeong et al (2018) Activation of temperature-sensitive TRPV1-like receptors in ARC POMC neurons reduces food intake. PLoS Biol 16 e2004399 PMID: 29689050
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该领域的文献
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。
Peptides Involved in Appetite Modulation Scientific Review
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.