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533928 REV-ERB Agonist, SR10067 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₃₁H₃₁NO₃

Products

Catalog NumberPackaging Qty/Pack
5.33928.0001 Glass bottle 10 mg
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
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 Identification Number
Catalog Number GTIN
5.33928.00014055977281613

Documentation

REV-ERB Agonist, SR10067 - 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
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.