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S2694

Sigma-Aldrich

SB-408124

≥98% (HPLC), solid

Synonym(s):

N-(6,8-Difluoro-2-methyl-4-quinolinyl)-N′-[4-(dimethylamino)phenyl]urea

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About This Item

Empirical Formula (Hill Notation):
C19H18F2N4O
CAS Number:
288150-92-5
Molecular Weight:
356.37
MDL number:
MFCD06411575
UNSPSC Code:
51111800
PubChem Substance ID:
329824523
NACRES:
NA.77

Assay

≥98% (HPLC)

form

solid

color

off-white

solubility

DMSO: >10 mg/mL

originator

GlaxoSmithKline

storage temp.

2-8°C

SMILES string

CN(C)c1ccc(NC(=O)Nc2cc(C)nc3c(F)cc(F)cc23)cc1

InChI

1S/C19H18F2N4O/c1-11-8-17(15-9-12(20)10-16(21)18(15)22-11)24-19(26)23-13-4-6-14(7-5-13)25(2)3/h4-10H,1-3H3,(H2,22,23,24,26)

InChI key

JTARFZSNUAGHRB-UHFFFAOYSA-N

Application

SB-408124 was used to block orexin A-mediated cardiovascular effects in rats. It was used to study block the increase of endogenous glucose production mediated by bicuculline in rats.

Biochem/physiol Actions

SB-408124 blocks the orexin type 1 receptor that stimulates the production of stress hormone in hypothalamus. It blocks orexin A-induced increase in arterial pressure and elevation of heart rate in rats. SB-408124 modulates phrenic nerve activity that is important in respiration.
SB 408124 is an OX1 orexin receptor antagonist.

Features and Benefits

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Legal Information

Sold for research purposes under agreement from Glaxo­Smith­Kline

Pictograms

Exclamation mark
GHS07

Signal Word

Warning

Hazard Statements

H315,H319,H335

Hazard Classifications

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

Target Organs

Respiratory system

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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(+)-Bicuculline ≥97.0% (TLC)

Sigma-Aldrich

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(+)-Bicuculline

Willis K Samson et al.
American journal of physiology. Regulatory, integrative and comparative physiology, 292(1), R382-R387 (2006-08-12)
Hypocretin/orexin acts pharmacologically in the hypothalamus to stimulate stress hormone secretion at least in part by an action in the hypothalamic paraventricular nucleus, where the peptide's receptors have been localized. In addition, orexin acts in the brain to increase sympathetic
Andrea Corcoran et al.
Advances in experimental medicine and biology, 669, 109-113 (2010-03-11)
Release of hypocretins (orexins) by neurons in the lateral hypothalamus is an important contributor to arousal state, thermoregulation, feeding behavior, and has recently been proposed to play a role in breathing and central chemosensitivity. Using the in situ arterially perfused
Chun-Xia Yi et al.
Diabetes, 58(9), 1998-2005 (2009-07-14)
The hypothalamic neuropeptide orexin influences (feeding) behavior as well as energy metabolism. Administration of exogenous orexin-A into the brain has been shown to increase both food intake and blood glucose levels. In the present study, we investigated the role of
Kaiyu Xu et al.
Nature communications, 11(1), 3594-3594 (2020-07-19)
Circular RNAs (circRNAs) are abundant in mammalian brain and some show age-dependent expression patterns. Here, we report that circGRIA1, a conserved circRNA isoform derived from the genomic loci of α-mino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor subunit Gria1, shows an age-related and

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