5.33928

REV-ERB Agonist, SR10067

• Synonim(y): REV-ERB Agonist, SR10067, (3-((4-(Tert-butoxy)phenoxy)methyl)-3,4-dihydroisoquinolin-2(1H)-yl)(naphthalen-1-yl)methanone
• Wzór empiryczny (zapis Hilla): C₃₁H₃₁NO₃
• Numer CAS: 1380548-02-6
• Masa cząsteczkowa: 465.58
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Próba: ≥98% (HPLC)
• Poziom jakości: 100
• Postać: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: white
• rozpuszczalność: DMSO: 8 mg/mL
• temp. przechowywania: −20°C

Opis

Opis ogólny

A 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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
REV-ERB

Reversible: yes

Target IC₅₀: 170 nM for REV-ERB&alpha

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Inne uwagi

Banerjee, S., et al. 2014. Nat. Comm.5, 5759.

Informacje prawne

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable