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

A cell-permeable, selective, brain permeant, potent, high-affinity agonist of REV-ERB (IC₅₀ = 170 and 160 nM for REV-ERB alpha and beta, respectively

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: (3-((4-(Tert-butoxy)phenoxy)methyl)-3,4-dihydroisoquinolin-2(1H)-yl)(naphthalen-1-yl)methanone

Primary Target: REV-ERB
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533928
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
1380548-02-6C₃₁H₃₁NO₃

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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
      Applications
      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
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalog Number GTIN
      5.33928.0001 04055977281613

      Documentation

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

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Banerjee, S., et al. 2014. Nat. Comm. 5, 5759.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision25-June-2016 JSW
      Synonyms(3-((4-(Tert-butoxy)phenoxy)methyl)-3,4-dihydroisoquinolin-2(1H)-yl)(naphthalen-1-yl)methanone
      DescriptionA 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.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1380548-02-6
      Chemical formulaC₃₁H₃₁NO₃
      Purity≥98% by HPLC
      SolubilityDMSO (8 mg/ml)
      Storage Protect from light
      -20°C
      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.
      Toxicity Standard Handling
      ReferencesBanerjee, S., et al. 2014. Nat. Comm. 5, 5759.