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Submit ReviewSB 408124
Description: Selective non-peptide OX1 antagonist
Chemical Name: N-(6,8-Difluoro-2-methyl-4-quinolinyl)-N'-[4-(dimethylamino)phenyl]urea
Purity: ≥98% (HPLC)
Biological Activity for SB 408124
SB 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.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Technical Data for SB 408124
| M. Wt | 356.37 |
| Formula | C19H18F2N4O |
| Storage | Store at RT |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SB 408124
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 35.64 | 100 |
Preparing Stock Solutions for SB 408124
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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 |
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Product Datasheets for SB 408124
References for SB 408124
References are publications that support the biological activity of the product.
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.
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Keywords: SB 408124, SB 408124 supplier, Selective, non-peptide, OX1, antagonists, Orexin1, Receptors, SB408124, GlaxoSmithKline, GSK, Receptor, 1963, Tocris Bioscience
2 Citations for SB 408124
Citations are publications that use Tocris products. Selected citations for SB 408124 include:
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
Do you know of a great paper that uses SB 408124 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.