GLPBio

SR 8278

Catalog No.: GC15275Purity:>99.50%
COASDSData Sheet
SR 8278 is an antagonist of the nuclear receptor REV-ERBα that can inhibit the transcription of REV-ERBα with an EC50 value of 0.47μM.

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SR 8278
Cas No.: 1254944-66-5
10mM (in 1mL DMSO)In Stock
$84.00
1
1mgIn Stock
$48.00
1
5mgIn Stock
$105.00
1
10mgIn Stock
$168.00
1
25mgIn Stock
$279.00
1
50mgIn Stock
$410.00
1
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Description

SR 8278 is an antagonist of the nuclear receptor REV-ERBα that can inhibit the transcription of REV-ERBα with an EC50 value of 0.47μM[1]. SR 8278 can be used to regulate metabolism in vivo, study biological rhythms, and treat mood disorders caused by Parkinson's disease[2, 3]. SR 8278 can effectively enhance the tear secretion function of jet-lagged mice by targeting NR1D1 inhibition[4].

In vitro, SR 8278 (50μM) pretreatment of HaCaT keratinocytes for 24h can protect keratinocytes from UVB radiation damage, but can make keratinocytes sensitive to UVA radiation and produce reactive oxygen species[5].

In vivo, SR 8278 (20μg/mouse) was slowly injected into the ventral tegmental area (VTA) of the midbrain to treat Parkinson's disease mice, which restored the emotion-related behavioral defects exhibited by the mice and restored the binding activity of REV-ERBα and NURR1[3]. SR 8278 (5mg/kg) was intraperitoneally injected into rats with acute lung injury (ALI) induced by ischemia-reperfusion (IR). It completely abolished the protective effect of SR9009 in IR-ALI and reversed the protective mechanisms of SR9009, including reducing pulmonary edema, inhibiting the production of inflammatory factors in bronchoalveolar lavage fluid (BALF), and reducing the accumulation of nuclear NF-κB p65 in lung tissue[6].

References:
[1] Kojetin D, Wang Y, Kamenecka T M, et al. Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB[J]. ACS chemical biology, 2011, 6(2): 131-134.
[2] Dong D, Sun H, Wu Z, et al. A validated ultra-performance liquid chromatography-tandem mass spectrometry method to identify the pharmacokinetics of SR8278 in normal and streptozotocin-induced diabetic rats[J]. Journal of Chromatography B, 2016, 1020: 142-147.
[3] Kim J, Park I, Jang S, et al. Pharmacological rescue with SR8278, a circadian nuclear receptor REV-ERBα antagonist as a therapy for mood disorders in Parkinson's disease[J]. Neurotherapeutics, 2022, 19(2): 592-607.
[4] Huang S, QI D, Pei X, et al. Transcriptomic analysis of SR8278 improving lacrimal gland dysfunction in-duced by jet lag in mice[J]. Recent Advances in Ophthalmology, 2024: 264-269.
[5] Cvammen W, Kemp M G. The REV‐ERB antagonist SR8278 modulates keratinocyte viability in response to UVA and UVB radiation[J]. Photochemistry and Photobiology, 2024, 100(6): 1864-1873.
[6] Chu S J, Liao W I, Pao H P, et al. Targeting Rev-Erbα to protect against ischemia-reperfusion-induced acute lung injury in rats[J]. Respiratory Research, 2023, 24(1): 247.

Protocol

Cell experiment [1]:

Cell lines

HaCaT keratinocytes

Preparation Method

HaCaT cells were pre-treated with DMSO vehicle, SR 8278 (50μM), KS15 (50μM), or both KS15 and SR 8278 (KS+SR) for 24h before exposure to the indicated fluences of UVB radiation. MTT assays were performed 3 days later to determine relative viability.

Reaction Conditions

50μM; 24h

Applications

The REV-ERB inhibitor SR 8278 protects keratinocytes against UVB radiation.

Animal experiment [2]:

Animal models

Sprague-Dawley rats

Preparation Method

The present study employed a randomized experimental design in which rats were assigned to one of eight groups. These included a control group that received DMSO, a drug control group that received 50mg/kg of SR9009 (i.p.), a group subjected to lung IR, and three groups that received different doses of SR9009 (12.5mg, 25mg, or 50mg/kg) along with lung IR, IR+SR8278 (5mg/kg), or IR+SR 8278 (5mg/kg)+SR9009 (50mg/kg) group. To facilitate intraperitoneal injection, SR9009 was dissolved in 0.5% DMSO and administered 60 min before inducing lung IR. In the IR + SR 8278 + SR9009 group, rats were pretreated with SR 8278 for 30min prior to SR9009 injection. Lung IR was induced by stopping ventilation and perfusion, leading to ischemia, and then maintaining the lungs in a deflated state for 40min, followed by 60min of ventilation and perfusion. In contrast, the control group received perfusate alone for 100min.

Dosage form

5mg/kg; i.p.

Applications

SR 8278 abolished the protective effects of SR9009 in IR-ALI. In this model, SR9009 had previously demonstrated a dose-dependent reduction in lung edema, along with significant inhibition of TNF-α, IL-6, and CINC-1 production in BALF. Additionally, SR9009 restored suppressed IκB-α levels and reduced nuclear NF-κB p65 accumulation in lung tissues. It also mitigated IR-induced apoptosis and suppressed MAPK activation in injured lung tissue. However, SR 8278 treatment completely reversed these protective mechanisms.

References:
[1] Cvammen W, Kemp M G. The REV?ERB antagonist SR8278 modulates keratinocyte viability in response to UVA and UVB radiation[J]. Photochemistry and Photobiology, 2024, 100(6): 1864-1873.
[2]Chu S J, Liao W I, Pao H P, et al. Targeting Rev-Erbα to protect against ischemia-reperfusion-induced acute lung injury in rats[J]. Respiratory Research, 2023, 24(1): 247.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
1254944-66-5
Chemical Name
(S)-ethyl 2-(5-(methylthio)thiophene-2-carbonyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate
SMILES
O=C([C@H]1N(C(C2=CC=C(SC)S2)=O)CC3=CC=CC=C3C1)OCC
Molecular Formula
C18H19NO3S2
Molecular Weight
361.48
Solubility
≤15mg/ml in ethanol;≤10mg/ml in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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