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SR9011

Catalog No.
B1768
REV-ERB-α/β agonist
Grouped product items
SizePriceStock Qty
2mg
$126.00
In stock
5mg
$252.00
In stock
10mg
$360.00
In stock
50mg
$1,350.00
In stock
100mg
$1,890.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

IC50: 790 nM for REV-ERB-α; 560 nM for REV-ERB-β

SR9011 is a REV-ERB-α/β agonist.

REV-ERB nuclear receptors have a critical role in feedback regulation of the circadian oscillator. Both Bmal1 and Clock are direct REV-ERB target genes and loss of REV-ERB-α alters circadian behaviour.

In vitro: SR9011 dose-dependently increased the REV-ERB-dependent repressor activity assessed in HEK293 cells. In addition, SR9011 potently and efficaciously suppressed transcription in a cotransfection assay using full-length REV-ERB-a along with a luciferase reporter driven by the Bmal1 promoter. SR9011 also suppressed the expression of BMAL1 messenger RNA in HepG2 cells in a REV-ERB-a/b-dependent manner. Moreover, SR9011 inhibited the activity of the SCNclock, with reversible inhibition of circadian oscillations [1].

In vivo: In the mice under constant darkness conditions, it was observed that the SR9011-dependent decrease in wheel running behaviour was dose-dependent and that the potency (half-maximum effective dose 56 mg/kg) was similar to the potency of SR9011-mediated suppression of a REV-ERB responsive gene, Srebf1, in vivo. Moreover, Tau was not affected by treatment with SR9011, and the recovery after the drug to resume the normal rhythm was similar to the effect observed after removal of the drug from the SCN explants [1].

Clinical trial: Up to now, SR9011 is still in the preclinical development stage.

Reference:
[1] Solt LA,Wang Y,Banerjee S,Hughes T,Kojetin DJ,Lundasen T,Shin Y,Liu J,Cameron MD,Noel R,Yoo SH,Takahashi JS,Butler AA,Kamenecka TM,Burris TP.  Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. Nature.2012 Mar 29;485(7396):62-8.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt479.04
Cas No.1379686-29-9
FormulaC23H31ClN4O3S
Solubility≥47.9mg/mL in DMSO
Chemical Name3-(((4-chlorobenzyl)((5-nitrothiophen-2-yl)methyl)amino)methyl)-N-pentylpyrrolidine-1-carboxamide
SDFDownload SDF
Canonical SMILESCCCCCNC(N1CCC(C1)CN(CC(S2)=CC=C2[N+]([O-])=O)CC3=CC=C(Cl)C=C3)=O
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

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