249889-64-3
Chemical Structure
SB-334867
Synonym(s): SB 334867A
- No. CAS: 249889-64-3
- Formula:C17H14ClN5O2
- Molecular Weight:355.78
IUPAC Name: 1-(2-methylbenzo[d]oxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea hydrochloride
InChIKey: BKZHSJNLPPAJKB-UHFFFAOYSA-N
SMILES: O=C(NC1=CC(OC(C)=N2)=C2C=C1)NC3=CC=NC4=CC=CN=C43.Cl
Biological Activity: SB-334867 (SB 334867A) is an excellent,selective and blood-brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively[1]. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo[2][3].
| Referencia número | Nombre del producto | Pureza | Descripciòn | Pricing | |||||||||||||||||||
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SB-334867 | 99.08% | SB-334867 (SB 334867A) is an excellent,selective and blood-brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo. | ||||||||||||||||||||
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SB-334867 (Standard) | ≥98% | SB-334867 (Standard) is the analytical standard of SB-334867. This product is intended for research and analytical applications. SB-334867 (SB 334867A) is an excellent,selective and blood-brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo. | ||||||||||||||||||||
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SB-200646A | 99.14% | SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo. | ||||||||||||||||||||
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SB-200646 | 98.38% | SB-200646 is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646 is orally active and has electrophysiological and anxiolytic properties in vivo. | ||||||||||||||||||||
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SB-334867 free base | 99.88% | SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo. | ||||||||||||||||||||
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Surfen | Surfen is a potent heparan sulfate antagonist. Surfen inhibits FGF2 binding and signal transduction. Surfen binds to glycosaminoglycans and reduces tau hyperphosphorylation. Surfen inhibits the activity of recombinant uronyl 2-O-sulfotransferase with an IC50 of approximately 2 μM. Surfen inhibits HSV-1 viral infection. Surfen inhibits neural differentiation, delays remyelination, and alleviates EAE. | |||||||||||||||||||||
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Surfen dihydrochloride | 99.93% | Surfen dihydrochloride is a potent heparan sulfate antagonist. Surfen inhibits FGF2 binding and signal transduction. Surfen binds to glycosaminoglycans and reduces tau hyperphosphorylation. Surfen dihydrochloride inhibits the activity of recombinant uronyl 2-O-sulfotransferase with an IC50 of approximately 2 μM. Surfen dihydrochloride inhibits HSV-1 viral infection. Surfen dihydrochloride inhibits neural differentiation, delays remyelination, and alleviates EAE. | ||||||||||||||||||||
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RF03176 | RF03176 is an aquaporin-9 (AQP-9) inhibitor, also exhibiting moderate inhibition effects on mAQP3 and mAQP7. RF03176 shows no activity against mAQP8. | |||||||||||||||||||||
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STING-IN-7 | 98.29% | STING-IN-7 is a potent STING inhibitor with an IC50 of 11.5 nM. STING-IN-7 can inhibit the phosphorylation of STING, IRF3, and TBK1. STING-IN-7 can be used in the research of autoimmune and inflammatory diseases. | ||||||||||||||||||||
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CJ28 | 99.21% | CJ28 is a cortisol biosynthesis inhibitor that significantly inhibits basal and stimulated cortisol production in human adrenal carcinoma cell lines. CJ28 exhibits inhibitory effects by reducing steroidogenesis and de novo cholesterol biosynthesis. | ||||||||||||||||||||
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SB-408124 | 98.93% | SB-408124 is a non-peptide OX1 receptor antagonist with Kis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 exhibits 50-fold selectivity over OX2 receptor. | ||||||||||||||||||||
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SB-408124 Hydrochloride (Standard) | ≥98% | SB-408124 (Hydrochloride) (Standard) is the analytical standard of SB-408124 (Hydrochloride). This product is intended for research and analytical applications. SB-408124 Hydrochloride is a selective non-peptide orexin receptor 1 (OX1) receptor antagonist with Kis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 Hydrochloride exhibits 50-fold selectivity over OX2 receptor. | ||||||||||||||||||||
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References
- [1]. Porter RA, et al. 1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.Bioorg Med Chem Lett. 2001 Jul 23;11(14):1907-10. [Content Brief]
- [2]. Łupina M, et al. SB-334867 (an Orexin-1 Receptor Antagonist) Effects on Morphine-Induced Sensitization in Mice-a View on Receptor Mechanisms. [Content Brief]
- [3]. Anderson RI, et al. Orexin-1 and orexin-2 receptor antagonists reduce ethanol self-administration in high-drinking rodent models.Front Neurosci. 2014 Feb 25;8:33. [Content Brief]