SB-334867 - CAS 249889-64-3
Catalog number: 249889-64-3
Category: Inhibitor
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Molecular Formula:
C17H13N5O2
Molecular Weight:
319.32
COA:
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Targets:
Orexin Receptor (OX Receptor)
Description:
SB-334867, with sedative and anorectic effects, it is the first non-peptide selective antagonist of orexin receptor subtype OX1 (pKb= 7.2) with 50 -fold selectivity for OX1 over OX2 receptors. in vitro: inhibited the orexin-A (10 nM) and orexin-B (100 nM)
Purity:
>99 %
Appearance:
Solid powder
Synonyms:
1-(2-methyl-1,3-benzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea 1-(2-methylbenzoxazol-6-yl)-3-(1,5)naphthyridin-4-yl urea 1-(2-methylbenzoxazol-6-yl)-3-(1,5)naphthyridin-4-yl urea hydrochloride SB 334867-A SB 334867A SB-334867 SB-334867-A SB-334867A SB3348
Solubility:
Soluble in DMSO
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -123℃ for long term (months to years).
MSDS:
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Shelf Life:
2 years
InChIKey:
AKMNUCBQGHFICM-UHFFFAOYSA-N
InChI:
1S/C17H13N5O2/c1-10-20-12-5-4-11(9-15(12)24-10)21-17(23)22-14-6-8-18-13-3-2-7-19-16(13)14/h2-9H,1H3,(H2,18,21,22,23)
Canonical SMILES:
CC1=NC2=C(O1)C=C(C=C2)NC(=O)NC3=C4C(=NC=C3)C=CC=N4
1.Orexins depolarize rostral ventrolateral medulla neurons and increase arterial pressure and heart rate in rats mainly via orexin 2 receptors.
Huang SC1, Dai YW, Lee YH, Chiou LC, Hwang LL. J Pharmacol Exp Ther. 2010 Aug;334(2):522-9. doi: 10.1124/jpet.110.167791. Epub 2010 May 21.
An injection of orexin A or B into the cisterna magna or the rostral ventrolateral medulla (RVLM), where bulbospinal vasomotor neurons are located, elevated arterial pressure (AP) and heart rate (HR). We examined how orexins affected RVLM neurons to regulate cardiovascular functions by using in vitro recordings of neuronal activity of the RVLM and in vivo measurement of cardiovascular functions in rats. Orexin A and B concentration-dependently depolarized RVLM neurons. At 100 nM, both peptides excited 42% of RVLM neurons. Tetrodotoxin failed to block orexin-induced depolarization. In the presence of N-(2-methyl-6-benzoxazolyl)-N'-1, 5-naphthyridin-4-yl urea (SB-334867), an orexin 1 receptor (OX(1)R) antagonist, orexin A depolarized 42% of RVLM neurons with a smaller, but not significantly different, amplitude (4.9 +/- 0.8 versus 7.2 +/- 1.1 mV). In the presence of (2S)-1- (3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-1-butanone hydrochloride (TCS OX2 29), an orexin 2 receptor (OX(2)R) antagonist, orexin A depolarized 25% of RVLM neurons with a significantly smaller amplitude (1.
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CAS 249889-64-3 SB-334867

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