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533928 REV-ERB Agonist, SR10067 - CAS 1380548-02-6 - Calbiochem

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CAS #Empirical Formula
1380548-02-6C₃₁H₃₁NO₃

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5.33928.0001
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      Description
      OverviewA cell-permeable, bioavailable, tetrahydroisoquinolin amide that acts as a selective, potent, and high-affinity agonist of REV-ERB (IC50 = 170 nM for REV-ERBα and IC50 = 160 nM for REV-ERBβ in a REV-ERB ligand-binding domain co-transfection assay). Able to cross the blood brain barrier and remain above the IC50 value even after 6 h (30 mg/kg, i.p.). Displays minimal activities against a wide of other receptors, ion channels, and transporters when screened at 20 µM. Shown to induce wakefulness and suppress circadian wheel-running activity (ED50 = 20 mg/kg injected at Zeitgeiber time 6 (ZT6)) in mice. Reduces slow-wave sleep (SWS) and REM sleep when injected at ZT6 with decreased duration and reduces the number of episodes and duration of REM sleep. Also shown to reduce anxiety-like behavior in the marble-burying assay.
      Catalogue Number533928
      Brand Family Calbiochem®
      Synonyms(3-((4-(Tert-butoxy)phenoxy)methyl)-3,4-dihydroisoquinolin-2(1H)-yl)(naphthalen-1-yl)methanone
      DescriptionREV-ERB Agonist, SR10067
      References
      ReferencesBanerjee, S., et al. 2014. Nat. Comm. 5, 5759.
      Product Information
      CAS number1380548-02-6
      FormWhite solid
      Hill FormulaC₃₁H₃₁NO₃
      Chemical formulaC₃₁H₃₁NO₃
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetREV-ERB
      Primary Target IC<sub>50</sub>170 nM for REV-ERB&alpha
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Référence GTIN
      5.33928.0001 04055977281613