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Merck
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Documenti fondamentali

SML2067

Sigma-Aldrich

SR9011

≥98% (HPLC)

Sinonimo/i:

3-[[[(4-Chlorophenyl)methyl][(5-nitro-2-thienyl)methyl]amino]methyl]-N-pentyl-1-pyrrolidinecarboxamide

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About This Item

Formula empirica (notazione di Hill):
C23H31ClN4O3S
Numero CAS:
1379686-29-9
Peso molecolare:
479.04
Codice UNSPSC:
12352200
NACRES:
NA.77

Saggio

≥98% (HPLC)

Stato

powder

Colore

white to beige

Solubilità

DMSO: 2 mg/mL, clear

Temperatura di conservazione

−20°C

Stringa SMILE

[s]1c(ccc1CN(CC3CN(CC3)C(=O)NCCCCC)Cc2ccc(cc2)Cl)[N+](=O)[O-]

InChI

PPUYOYQTTWJTIU-UHFFFAOYSA-N

Applicazioni

SR9011 has been used as a nuclear receptor subfamily 1 group D member 1 (NR1D1) receptor agonist:
  • to study its effects on microglial immune-metabolism
  • to study its effects on insulin secretion from human type 2 diabetes islet cells
  • to study its effects on thyroid-stimulating hormone β (TSHβ) gene expression

Azioni biochim/fisiol

REV-ERBα/β agonist that promotes REV-ERB-dependent repressor activity both in cultures and in mice in vivo.
SR9011 is a potent nuclear receptor REV-ERB agonist (EC50 of REV-ERBα- and REV-ERBβ-dependent repressor activity = 790 and 560 nM, respectively, by cell-based reporter assay) that stimulates REV-ERB-dependent target genes suppression both in cultures in vitro and in mice in vivo (100 mg/kg i.p., b.i.d.) without activity toward a panel of 46 other nuclear receptors. SR9011 is shown to modulate circadian behavior by suppressing the transcription factors BMAL1 (brain and muscle ARNT-like protein 1) and CLOCK (circadian locomotor output cycles kaput) as well as induce energy expenditure and weight loss by regulating genes involved in lipid and glucose metabolism in mice in vivo with good bioavailabiilty (plasma conc. = 0.53 and 15.3 μM 2 hr post 10 or 100 mg/kg i.p. dosage; brain conc. = 0.24 μM 2 hr post 10 mg/kg i.p.), while its structure analog GSK4112 shows no plasma exposure.

Pittogrammi

Exclamation mark
GHS07

Avvertenze

Warning

Indicazioni di pericolo

H315,H319

Classi di pericolo

Eye Irrit. 2 - Skin Irrit. 2

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

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Certificati d'analisi (COA)

Lot/Batch Number

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Laura A Solt et al.
Nature, 485(7396), 62-68 (2012-03-31)
Synchronizing rhythms of behaviour and metabolic processes is important for cardiovascular health and preventing metabolic diseases. The nuclear receptors REV-ERB-α and REV-ERB-β have an integral role in regulating the expression of core clock proteins driving rhythms in activity and metabolism.
Irene O Aninye et al.
The Journal of biological chemistry, 289(24), 17070-17077 (2014-05-06)
Thyroid hormones (TH) are critical for development, growth, and metabolism. Circulating TH levels are tightly regulated by thyroid-stimulating hormone (TSH) secretion within the hypothalamic-pituitary-thyroid axis. Although circadian TSH secretion has been well documented, the mechanism of this observation remains unclear.
Sadichha Sitaula et al.
Biochemical pharmacology, 131, 68-77 (2017-02-19)
REV-ERBα and REV-ERBβ are heme regulated nuclear receptors that are known to regulate metabolic pathways. We previously demonstrated that treatment of mice with synthetic REV-ERB agonists suppressed plasma cholesterol levels and the hepatic levels of the rate limiting enzyme in
Ryota Nakazato et al.
Glia, 65(1), 198-208 (2016-10-12)
Similar to neurons, microglia have an intrinsic molecular clock. The master clock oscillator Bmal1 modulates interleukin-6 upregulation in microglial cells exposed to lipopolysaccharide. Bmal1 can play a role in microglial inflammatory responses. We previously demonstrated that gliotransmitter ATP induces transient

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