Name: SR9011
Price: 271.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    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.
- Properties
  - Categories
    
    REV-ERB-α/β agonist
    
    Alternative Name
    
    3-(((4-chlorobenzyl)((5-nitrothiophen-2-yl)methyl)amino)methyl)-N-pentylpyrrolidine-1-carboxamide
    
    CAS Number
    
    1379686-29-9
    
    Molecular Formula
    
    C23H31ClN4O3S
    
    Molecular Weight
    
    479.04
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥47.9 mg/mL in DMSO; insoluble in H2O; ≥59.7 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    CCCCCNC(N1CCC(C1)CN(CC(S2)=CC=C2[N+]([O-])=O)CC3=CC=C(Cl)C=C3)=O
    
    * For Research Use Only

Documents

COA (Certificate Of Analysis)

MSDS (Material Safety Data Sheet)

Datasheet

SR9011

SR9011

Background

Documents

We Also Recommend

Histamine Phosphate

Hydroxypropyl Cellulose

Ibandronate sodium