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Submit ReviewSB 674042
Description: Potent and selective non-peptide OX1 antagonist
Chemical Name: [5-(2-Fluorophenyl)-2-methyl-4-thiazolyl][2(S)-2-[(5-phenyl-1,3,4-oxadiazol-2-yl)methyl-1-pyrrolidinyl]methanone
Biological Activity for SB 674042
SB 674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd = 3.76 nM). Exhibits 100-fold selectivity for OX1 over OX2 receptors. Has no effect at serotonergic, dopaminergic, adrenergic or purinergic receptors. Inhibits orexin 1-induced Ca2+ mobilization in CHO-DG44 cells stably transfected with the OX1 receptor.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline.
Technical Data for SB 674042
| M. Wt | 448.51 |
| Formula | C24H21FN4O2S |
| Storage | Store at +4°C |
| CAS Number | 483313-22-0 |
| PubChem ID | 10204153 |
| InChI Key | HYBZWVLPALMACV-KRWDZBQOSA-N |
| Smiles | O=C(C2=C(C5=CC=CC=C5F)SC(C)=N2)N1[C@H](CC3=NN=C(C4=CC=CC=C4)O3)CCC1 |
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 674042
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 44.85 | 100 | |
| ethanol | 44.85 | 100 |
Preparing Stock Solutions for SB 674042
The following data is based on the product molecular weight 448.51. 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 | 2.23 mL | 11.15 mL | 22.3 mL |
| 5 mM | 0.45 mL | 2.23 mL | 4.46 mL |
| 10 mM | 0.22 mL | 1.11 mL | 2.23 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
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Product Datasheets for SB 674042
References for SB 674042
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
Ellis et al (2006) Orexin-1 receptor-cannabinoid CB1 receptor heterodimerization results in both ligand-dependent and -independent coordinated alterations of receptor localization and function. Biol.Chem. 281 38812 PMID: 17015451
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Keywords: SB 674042, SB 674042 supplier, Potent, selective, non, peptide, OX1, receptors, antagonists, orexin1, orexin-1, SB674042, Receptor, 4673, Tocris Bioscience
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Literature in this Area
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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.