5.33928

REV-ERB Agonist, SR10067

• 동의어(들): REV-ERB Agonist, SR10067, (3-((4-(Tert-butoxy)phenoxy)methyl)-3,4-dihydroisoquinolin-2(1H)-yl)(naphthalen-1-yl)methanone
• 실험식(Hill 표기법): C₃₁H₃₁NO₃
• CAS Number: 1380548-02-6
• Molecular Weight: 465.58
• MDL number: MFCD00000003
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 분석: ≥98% (HPLC)
• Quality Level: 100
• 양식: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: white
• solubility: DMSO: 8 mg/mL
• 저장 온도: −20°C

설명

일반 설명

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.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
REV-ERB

Reversible: yes

Target IC₅₀: 170 nM for REV-ERB&alpha

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

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

기타 정보

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

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable