SB 674042

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Cat.No. 4673 - SB 674042 | CAS No. 483313-22-0
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
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Biological Activity

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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 44.85 100
ethanol 44.85 100

Preparing Stock Solutions

The following data is based on the product molecular weight 448.51. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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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References

References are publications that support the products' biological activity.

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, supplier, Potent, selective, non, peptide, OX1, receptors, antagonists, orexin1, orexin-1, SB674042, OX1, Receptor, OX1, Receptor, Tocris Bioscience

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