Art. -Nr.: HY-14415

SR8278

17 Cited Publications

Kundenbewertung

Based on 17 publication(s) in Google Scholar

SR8278 is a REV-ERBα antagonist and inhibits the REV-ERBα transcriptional repression activity with an EC₅₀ of 0.47 μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm. SR8278 also can be used for the research of Duchenne muscular dystrophy and Alzheimer's disease.

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Reinheit: 99.89%
CAS. Nr.: 1254944-66-5
Formel: C₁₈H₁₉NO₃S₂
Molecular Weight:361.48

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

SR8278 Chemical Structure

CAS. Nr.: 1254944-66-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (17)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

EC50: 0.47 μM (REV-ERBα)^[1].

In Vitro

SR8278 has REV-ERBα transcriptional repression inhibitory activity with an EC₅₀ of 0.47μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SR8278 (slow microinjection; 20 μg/mouse) exerts antidepressant and anxiolytic effects in a circadian time-dependent manner in 6-OHDA-lesioned mice and restores the circadian rhythm of mood-related behaviors^[1].
SR8278 (slow microinjection; 20 μg/mouse) restores the binding activities of REV-ERBα and NURR1 to the tyrosine hydroxylase promoter and the induction of enrichment of the R/N motif, recognized by REV-ERBα and NURR1^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

6-OHDA-lesioned mice^[1]
Dosage:

20 μg/mouse
Administration:

slow microinjection; 20 μg/mouse
Result:

Recovered mood-related behavioral deficits shown in 6-OHDA-lesioned mice.
Altered remaining DAergic neuron specific transcription levels of REV-ERBα and Nurr1 in the VTA.
Restored antagonistic crosstalk of REV-ERBα and NURR1 binding activity to TH promoter and TH protein levels in VTA.
Induced enrichments of REV-ERBα and NURR1 binding motifs at dawn.

Chemical Information

CAS. Nr. 1254944-66-5
Appearance Solid
Molecular Weight 361.48
Formel C₁₈H₁₉NO₃S₂
Color White to light yellow
SMILES

CSC1=CC=C(C(N2C(C(OCC)=O)CC(C=CC=C3)=C3C2)=O)S1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (17)

All WBIn Vivo Efficacy StudyCell Imaging/StainingHistological Imaging/Staining

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Journal Impact Factor

Nat Commun

Deficiency of intestinal Bmal1 prevents obesity induced by high-fat feeding. [Abstract]

2021 Sep 7;12(1):5323. PMID: 34493722

SR8278 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Sep 7;12(1):5323. [Abstract]

Effects of SR8278 (100 mg/kg; i.g.; once daily for 4 weeks) on BMAL1 and DGAT2 expression in small intestine of HFD-fed mice.

SR8278 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Sep 7;12(1):5323. [Abstract]

SR8278 (100 mg/kg; i.g.; once daily for 4 weeks) significantly increased body weight gain, serum/hepatic/ intestinal TAG and FFA levels in HFD-fed mice.
Int J Oral Sci

Circadian disruption by simulated shift work aggravates periodontitis via orchestrating BMAL1 and GSDMD-mediated pyroptosis. [Abstract]

2025 Feb 25;17(1):14. PMID: 40000642

SR8278 purchased from MedChemExpress. Usage Cited in: Int J Oral Sci. 2025 Feb 25;17(1):14. [Abstract]

SR8278 (2.5 μM) increased the protein levels of BMAL1, NLRP3, and pro-CASPASE1 and downregulated the full length and N-terminal cleavage of GSDMD in mGFs.

SR8278 purchased from MedChemExpress. Usage Cited in: Int J Oral Sci. 2025 Feb 25;17(1):14. [Abstract]

SR8278 (2.5 μM) ameliorated P. gingivalis LPS-induced death of mGFs.

SR8278 purchased from MedChemExpress. Usage Cited in: Int J Oral Sci. 2025 Feb 25;17(1):14. [Abstract]

SR8278 (500 μM; 110 μL; i.p.; ZT 4) injection reduced GSDMD levels and alleviated alveolar bone resorption and periodontal destruction exacerbated by circadian disruption.
J Neuroinflammation

The circadian clock protein Rev-erbα provides neuroprotection and attenuates neuroinflammation against Parkinson's disease via the microglial NLRP3 inflammasome. [Abstract]

2022 Jun 6;19(1):133. PMID: 35668454
J Orthop Translat

Inhibiting the REV-ERBα expression protects against mechanical overloading-induced cartilage clock disruption and osteoarthritis progression. [Abstract]

2025 Jun 18:53:112-125. PMID: 40606845
Int J Mol Med

Melatonin inhibits RANKL‑induced osteoclastogenesis through the miR‑882/Rev‑erbα axis in Raw264.7 cells. [Abstract]

2021 Feb;47(2):633-642. PMID: 33416111
Cell Rep

IRE1α regulates macrophage phagocytosis in immune thrombocytopenia through NR1D1 mRNA decay and lysosomal biogenesis. [Abstract]

2026 Mar 12;45(3):117083. PMID: 41824452
J Pineal Res

Melatonin Ameliorates Circadian Disruption-Associated Dry Eye via Modulation of BMAL1-REV-ERBα-IL-17 Axis and Ocular Surface Microbiota Homeostasis. [Abstract]

2025 Sep;77(5):e70076. PMID: 40936475
Br J Pharmacol

Targeted inhibition of Rev-erb-α/β limits ferroptosis to ameliorate folic acid-induced acute kidney injury. [Abstract]

2021 Jan;178(2):328-345. PMID: 33068011
Int Immunopharmacol

Berberine alleviates LPS-induced inflammatory response by targeted activation of NR1D1 in bovine endometrial epithelial cells. [Abstract]

2026 Aug 15:183:116858. PMID: 42150288
J Clin Endocrinol Metab

Overexpression of NR1D1 Portends Disease Recurrence in Thyroid Cancer. [Abstract]

2025 Mar 17;110(4):991-1002. PMID: 39359072
Mol Med Rep

Rev‑erbα: The circadian guardian against NLRP3‑driven liver fibrosis. [Abstract]

2025 Oct;32(4):270. PMID: 40709400
J Cell Mol Med

Melatonin inhibits osteoclastogenesis via RANKL/OPG suppression mediated by Rev-Erbα in osteoblasts. [Abstract]

2022 Jul;26(14):4032-4047. PMID: 35726597
Cell Transplant

Olfactory Ensheathing Cell Ameliorate Neuroinflammation Following Spinal Cord Injury Through Upregulating REV-ERBα in Microglia. [Abstract]

2024 Jan-Dec:33:9636897241261234. PMID: 39068549
J Mol Histol

Circadian rhythm disruption affects cellular senescence through the BMAL1/CRY2/PER1 signaling pathway in periodontitis. [Abstract]

2026 Apr 16;57(3):141. PMID: 41989670
In Vitro Cell Dev Biol Anim

Clock genes are expressed in cementum and regulate the proliferation and mineralization of cementoblasts. [Abstract]

2023 Jan;59(1):76-84. PMID: 36790692

SR8278 purchased from MedChemExpress. Usage Cited in: In Vitro Cell Dev Biol Anim. 2023 Jan;59(1):76-84. [Abstract]

SR8278 promotes the expression of ALPL, BSP, OPN, RUNX2, and OSX signifcantly in OCCM-30 cells.
Heliyon

REV-ERBα inhibitor rescues MPTP/MPP+-induced ferroptosis of dopaminergic neuron through regulating FASN/SCD1 signaling pathway. [Abstract]

2024 Nov 15;10(23):e40388. PMID: 39654780
bioRxiv

2024 May 3.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (276.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7664 mL

13.8320 mL

27.6640 mL

5 mM

0.5533 mL

2.7664 mL

5.5328 mL

10 mM

0.2766 mL

1.3832 mL

2.7664 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.92 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.92 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.92 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Kojetin , et al. Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB. ACS Chem Biol. 2011 Feb 18;6(2):131-4. [Content Brief]

[2]. Dong D, 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 Chromatogr B Analyt Technol Biomed Life Sci. 2016 May 1;1020:142-7. [Content Brief]

[3]. Jeongah Kim, et al. Pharmacological Rescue with SR8278, a Circadian Nuclear Receptor REV-ERBα Antagonist as a Therapy for Mood Disorders in Parkinson's Disease. Neurotherapeutics. 2022 Mar;19(2):592-607. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7664 mL	13.8320 mL	27.6640 mL	69.1601 mL
	5 mM	0.5533 mL	2.7664 mL	5.5328 mL	13.8320 mL
	10 mM	0.2766 mL	1.3832 mL	2.7664 mL	6.9160 mL
	15 mM	0.1844 mL	0.9221 mL	1.8443 mL	4.6107 mL
	20 mM	0.1383 mL	0.6916 mL	1.3832 mL	3.4580 mL
	25 mM	0.1107 mL	0.5533 mL	1.1066 mL	2.7664 mL
	30 mM	0.0922 mL	0.4611 mL	0.9221 mL	2.3053 mL
	40 mM	0.0692 mL	0.3458 mL	0.6916 mL	1.7290 mL
	50 mM	0.0553 mL	0.2766 mL	0.5533 mL	1.3832 mL
	60 mM	0.0461 mL	0.2305 mL	0.4611 mL	1.1527 mL
	80 mM	0.0346 mL	0.1729 mL	0.3458 mL	0.8645 mL
	100 mM	0.0277 mL	0.1383 mL	0.2766 mL	0.6916 mL

Keywords

SR8278

17 Cited Publications

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SR8278

Metabolism/Protease Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Targeted Diversity Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) SR8278

Biologische Aktivität

Chemical Information

Publications (17)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SR8278

Metabolism/Protease Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Targeted Diversity Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) SR8278

Biologische Aktivität

Chemical Information

Publications (17)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SR8278 Related Classifications

HY-14415 Related Classifications