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Submit Review[Ala11,D-Leu15]-Orexin B is a highly potent and selective OX2 receptor agonist; displays 400-fold selectivity over OX1 receptors. EC50 values are 0.13 and 52 nM for human OX2 and OX1 receptors respectively.
分子量 | 2857.28 |
公式 | C120H206N44O35S |
序列 |
RSGPPGLQGRAQRLLQASGNHAAGILTM (Modification: Leu-15 = D-Leu, Met-28 = C-terminal amide) |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 532932-99-3 |
PubChem ID | 16201464 |
InChI Key | SURUUKNICBOUOQ-JNZZMZGCSA-N |
Smiles | [H]N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCSC)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。
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溶解性 | Soluble to 0.30 mg/ml in water |
参考文献是支持产品生物活性的出版物。
Asahi et al (2003) Development of an orexin-2 receptor selective agonist, [Ala11D-Leu15]orexin-B. Bioorg.Med.Chem.Lett. 13 111 PMID: 12467628
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关键词: [Ala11,D-Leu15]-Orexin B, [Ala11,D-Leu15]-Orexin B supplier, Potent, selective, OX2, receptor, agonists, Orexin2, Receptors, [Ala11D-Leu15]-OrexinB, Receptor, 2142, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 [Ala11,D-Leu15]-Orexin B 的部分引用包括:
Moore et al (2014) Effects of orexin 2 receptor activation on apnea in the C57BL/6J mouse. Respir Physiol Neurobiol 200 118 PMID: 24929062
Malherbe et al (2009) Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX(2) receptor. Br J Pharmacol 156 1326 PMID: 19751316
Guo and Feng (2012) OX2R activation induces PKC-mediated ERK and CREB phosphorylation. Exp Cell Res 318 2004 PMID: 22652455
Shahid et al (2012) Orexin A in rat rostral ventrolateral medulla is pressor, sympatho-excitatory, increases barosensitivity and attenuates the somato-sympathetic reflex. Br J Pharmacol 165 2292 PMID: 21951179
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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.