SR8278
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.89%
- No. CAS: 1254944-66-5
- Fòrmula: C18H19NO3S2
- Peso molecular:361.48
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) SR8278
More- Nat Commun. 2021 Sep 7;12(1):5323. [Abstract]
- Int J Oral Sci. 2025 Feb 25;17(1):14. [Abstract]
- J Neuroinflammation. 2022 Jun 6;19(1):133. [Abstract]
- J Orthop Translat. 2025 Jun 18:53:112-125. [Abstract]
- Int J Mol Med. 2021 Feb;47(2):633-642. [Abstract]
- Cell Rep. 2026 Mar 12;45(3):117083. [Abstract]
- J Pineal Res. 2025 Sep;77(5):e70076. [Abstract]
- Br J Pharmacol. 2021 Jan;178(2):328-345. [Abstract]
- Int Immunopharmacol. 2026 Aug 15:183:116858. [Abstract]
- J Clin Endocrinol Metab. 2025 Mar 17;110(4):991-1002. [Abstract]
- Mol Med Rep. 2025 Oct;32(4):270. [Abstract]
- J Cell Mol Med. 2022 Jul;26(14):4032-4047. [Abstract]
- Cell Transplant. 2024 Jan-Dec:33:9636897241261234. [Abstract]
- J Mol Histol. 2026 Apr 16;57(3):141. [Abstract]
- In Vitro Cell Dev Biol Anim. 2023 Jan;59(1):76-84. [Abstract]
- Heliyon. 2024 Nov 15;10(23):e40388. [Abstract]
- bioRxiv. 2024 May 3.
Customer Validation & Images
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Actividad biológica
EC50: 0.47 μM (REV-ERBα)[1].
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.
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.
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Animal Model:6-OHDA-lesioned mice[1]
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Dosage:20 μg/mouse
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Administration:slow microinjection; 20 μg/mouse
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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
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No. CAS 1254944-66-5
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Appearance Solid
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Peso molecular 361.48
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Fòrmula C18H19NO3S2
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Color White to light yellow
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SMILES
CSC1=CC=C(C(N2C(C(OCC)=O)CC(C=CC=C3)=C3C2)=O)S1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (17)
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Journal Impact Factor
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Most Recent
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Nat Commun
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.
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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.
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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
2025 Mar 17;110(4):991-1002. PMID: 39359072 -
Mol Med Rep
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.
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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 -
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
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