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SB 674042
Axon 2192
CAS:
483313-22-0
- Optical Purity: >99% e.e.
- Soluble in DMSO and EtOH
- MF: C24H21FN4O2S
- MW: 448.51
Description
Nonpeptide OX1 selective antagonist (Kd value 3.76 nM) with >100 fold selectivity over the OX2 receptor. SB 674042 displays no significant affinity for a range of serotonergic, dopaminergic, adrenergic and purinergic receptors at concentrations up to 10 μM.
SB 674042 was also shown to be a competitive, functional antagonist of the OX1 receptor in the calcium mobilisation assay using CHO-DG44_OX1 cell lines.
More Information
| Parent CAS No. | 483313-22-0 |
|---|---|
| Chemical Name | (S)-(5-(2-fluorophenyl)-2-methylthiazol-4-yl)(2-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)pyrrolidin-1-yl)methanone |
| SMILES | C(C1=C(C2=CC=CC=C2F)SC(C)=N1)(N1CCC[C@H]1CC1=NN=C(C2=CC=CC=C2)O1)=O |&1:18,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C24H21FN4O2S/c1-15-26-21(22(32-15)18-11-5-6-12-19(18)25)24(30)29-13-7-10-17(29)14-20-27-28-23(31-20)16-8-3-2-4-9-16/h2-6,8-9,11-12,17H,7,10,13-14H2,1H3/t17-/m0/s1 |
| InChiKey | HYBZWVLPALMACV-KRWDZBQOSA-N |
| CID | 10204153 |
| Short Description | OX1 antagonist |
References
- A. Heifetz et al. Study of Human Orexin-1 and -2 G-Protein-Coupled Receptors with Novel and Published Antagonists by Modeling, Molecular Dynamics Simulations, and Site-Directed Mutagenesis. Biochem. 2012, 51, 3178-3197.
- C.J. Langmead et al. Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br. J. Pharmacol. 2004, 141, 340-346.
- P. Malherbe et al. Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX2 receptor. Br. J. Pharmacol. 2009, 156, 1326-1341.
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