SR9011 is a potent nuclear receptor REV-ERB agonist (EC50 of REV-ERBalpha- and REV-ERBbeta-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 (100mg/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 15.3uM 2 hr post 10 or 100mg/kg i.p. dosage, brain conc. = 0.24uM 2 hr post 10mg/kg i.p.), while its structure analog GSK4112 shows no plasma exposure. Synonyms: 3-[[[(4-Chlorophenyl)methyl][(5-nitro-2-thienyl)methyl]amino]methyl]-N-pentyl-1-pyrrolidinecarboxamide CAS No: 1379686-29-9 Molecular Formula: C23H31ClN4O3S Molecular Weight: 479.04 Appearance: White to beige powder Purity: 98% (HPLC) Solubility: DMSO: 2mg/ml, clear Storage and Stability: Store at -20C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Molekulargewicht:
479.04
Reinheit:
98% (HPLC)
Formulierung:
White to beige powder
CAS Nummer:
[1379686-29-9]
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