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Submit ReviewSB 408124 is a selective non-peptide orexin OX1 receptor antagonist (Kb values are 21.7 and 1405 nM for human OX1 and OX2 receptors respectively). Blocks orexin-A induced grooming following oral administration in vivo.
Sold for research purposes under agreement from GlaxoSmithKline
分子量 | 356.37 |
公式 | C19H18F2N4O |
储存 | Store at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 288150-92-5 |
PubChem ID | 4331799 |
InChI Key | JTARFZSNUAGHRB-UHFFFAOYSA-N |
Smiles | CN(C)C1=CC=C(NC(=O)NC2=CC(C)=NC3=C(F)C=C(F)C=C23)C=C1 |
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 | 35.64 | 100 |
以下数据基于产品分子量 356.37。 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 |
---|---|---|---|
1 mM | 2.81 mL | 14.03 mL | 28.06 mL |
5 mM | 0.56 mL | 2.81 mL | 5.61 mL |
10 mM | 0.28 mL | 1.4 mL | 2.81 mL |
50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
参考文献是支持产品生物活性的出版物。
Langmead et al (2004) Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br.J.Pharmacol. 141 340 PMID: 14691055
Porter (2001) Advances in novel 7-TM receptors: non-peptide orexin-1 antagonists. Royal Society of Chemistry Meeting.
If you know of a relevant reference for SB 408124, please let us know.
关键词: SB 408124, SB 408124 supplier, Selective, non-peptide, OX1, antagonists, Orexin1, Receptors, SB408124, GlaxoSmithKline, GSK, Receptor, 1963, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 SB 408124 的部分引用包括:
Suo et al (2018) The Orexin-A-Regulated Akt/mTOR Pathway Promotes Cell Proliferation Through Inhibiting Apoptosis in Pancreatic Cancer Cells. Front Endocrinol (Lausanne) 9 647 PMID: 30429828
Urbałska et al (2012) Orexins/hypocretins acting at Gi protein-coupled OX 2 receptors inhibit cyclic AMP synthesis in the primary neuronal cultures. BMC Cancer 46 42561 PMID: 21547533
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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!
*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.