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MedKoo Cat#: 532782 | Name: SR8278
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

SR8278 is a rev-erbα antagonist. It inhibits Rev-Erbα transcriptional repression (EC50 = 0.47 μM) and blocks activity of Rev-Erbα agonist GSK 4112 in HEK293 cells. SR8278 increases expression of glucose-regulating genes, G6Pase and PEPCK in HepG2 cells.

Chemical Structure

SR8278
CAS#1254944-66-5

Theoretical Analysis

MedKoo Cat#: 532782

Name: SR8278

CAS#: 1254944-66-5

Chemical Formula: C18H19NO3S2

Exact Mass: 361.0806

Molecular Weight: 361.47

Elemental Analysis: C, 59.81; H, 5.30; N, 3.87; O, 13.28; S, 17.74

Price and Availability

Size Price Availability Quantity
50mg USD 550.00 2 Weeks
100mg USD 950.00 2 Weeks
200mg USD 1,650.00 2 Weeks
500mg USD 2,650.00 2 Weeks
1g USD 3,450.00 2 Weeks
2g USD 6,450.00 2 Weeks
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Related CAS #
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Synonym
SR8278; SR 8278; SR-8278.
IUPAC/Chemical Name
ethyl 2-{[5-(methylsulfanyl)thiophen-2-yl]carbonyl}-1,2,3,4-tetrahydroisoquinoline-3-carboxylate
InChi Key
UIEBLUZPSFAFOC-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H19NO3S2/c1-3-22-18(21)14-10-12-6-4-5-7-13(12)11-19(14)17(20)15-8-9-16(23-2)24-15/h4-9,14H,3,10-11H2,1-2H3
SMILES Code
O=C(C1N(C(C2=CC=C(SC)S2)=O)CC3=C(C=CC=C3)C1)OCC
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, DMF, and ethanol
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
SR8278 is an antagonist of REV-ERBα (EC50 = 0.47 µM), blocking activation of the receptor by the synthetic agonist GSK 4112.
In vitro activity:
SR8278 has limited utility for UV photoprotection in the skin and will likely cause phototoxicity in humans or mammals exposed to solar radiation. SR8278 promoted UVB viability, indicating that SR8278 is likely acting via other REV-ERB transcriptional targets. SR8278 also sensitized keratinocytes to light sources containing primarily UVA wavelengths of light likely due to the generation of toxic reactive oxygen species. Reference: Photochem Photobiol. 2024 Mar 8. https://pubmed.ncbi.nlm.nih.gov/38459721/
In vivo activity:
SR8278 is a potential drug for mood disorders related to circadian disturbances, namely sundowning syndrome, in Parkinson's disease. SR8278 exerted antidepressant and anxiolytic effects in a circadian time-dependent manner in 6-OHDA-lesioned mice and restored the circadian rhythm of mood-related behaviors. Also, SR8278 treatment restored the binding activities of REV-ERBα and NURR1 to the tyrosine hydroxylase promoter and the induction of enrichment of the R/N motif. Reference: Neurotherapeutics. 2022 Mar;19(2):592-607. https://pubmed.ncbi.nlm.nih.gov/35322351/
Solvent mg/mL mM comments
Solubility
DMF 15.0 41.50
DMSO 10.0 27.66
Ethanol 15.0 41.50
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 361.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Cvammen W, Kemp MG. The REV-ERB antagonist SR8278 modulates keratinocyte viability in response to UVA and UVB radiation. Photochem Photobiol. 2024 Mar 8. doi: 10.1111/php.13930. Epub ahead of print. PMID: 38459721. 2. Kojetin D, Wang Y, Kamenecka TM, Burris TP. Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB. ACS Chem Biol. 2011 Feb 18;6(2):131-4. doi: 10.1021/cb1002575. Epub 2010 Nov 10. PMID: 21043485; PMCID: PMC3042041. 3. Kim J, Park I, Jang S, Choi M, Kim D, Sun W, Choe Y, Choi JW, Moon C, Park SH, Choe HK, Kim K. 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. doi: 10.1007/s13311-022-01215-w. Epub 2022 Mar 23. Erratum in: Neurotherapeutics. 2022 May 2;: PMID: 35322351; PMCID: PMC9226214. 4. Dong D, Sun H, Wu Z, Wu B, Xue Y, Li Z. 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. doi: 10.1016/j.jchromb.2016.03.033. Epub 2016 Mar 26. PMID: 27038650.
In vitro protocol:
1. Cvammen W, Kemp MG. The REV-ERB antagonist SR8278 modulates keratinocyte viability in response to UVA and UVB radiation. Photochem Photobiol. 2024 Mar 8. doi: 10.1111/php.13930. Epub ahead of print. PMID: 38459721. 2. Kojetin D, Wang Y, Kamenecka TM, Burris TP. Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB. ACS Chem Biol. 2011 Feb 18;6(2):131-4. doi: 10.1021/cb1002575. Epub 2010 Nov 10. PMID: 21043485; PMCID: PMC3042041.
In vivo protocol:
1. Kim J, Park I, Jang S, Choi M, Kim D, Sun W, Choe Y, Choi JW, Moon C, Park SH, Choe HK, Kim K. 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. doi: 10.1007/s13311-022-01215-w. Epub 2022 Mar 23. Erratum in: Neurotherapeutics. 2022 May 2;: PMID: 35322351; PMCID: PMC9226214. 2. Dong D, Sun H, Wu Z, Wu B, Xue Y, Li Z. 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. doi: 10.1016/j.jchromb.2016.03.033. Epub 2016 Mar 26. PMID: 27038650.
1: Yang Y, Zhang X, Cai D, Zheng X, Zhao X, Zou JX, Zhang J, Borowsky AD, Dall'Era MA, Corey E, Mitsiades N, Kung HJ, Chen X, Li JJ, Downes M, Evans RM, Chen HW. Functional inversion of circadian regulator REV-ERBα leads to tumorigenic gene reprogramming. Proc Natl Acad Sci U S A. 2024 Oct 15;121(42):e2411321121. doi: 10.1073/pnas.2411321121. Epub 2024 Oct 9. PMID: 39383000; PMCID: PMC11494309. 2: Darmanto AG, Jan JS, Yen TL, Huang SW, Teng RD, Wang JY, Taliyan R, Sheu JR, Yang CH. Targeting Circadian Protein Rev-erbα to Alleviate Inflammation, Oxidative Stress, and Enhance Functional Recovery Following Brain Trauma. Antioxidants (Basel). 2024 Jul 25;13(8):901. doi: 10.3390/antiox13080901. PMID: 39199147; PMCID: PMC11351136. 3: Li X, Zhuang R, Lu Z, Wu F, Wu X, Zhang K, Wang M, Li W, Zhang H, Zhu W, Zhang B. Nobiletin promotes lipolysis of white adipose tissue in a circadian clock-dependent manner. J Nutr Biochem. 2024 Oct;132:109696. doi: 10.1016/j.jnutbio.2024.109696. Epub 2024 Aug 1. PMID: 39094217. 4: Rahman MH, Hegazy L. Mechanism of antagonist ligand binding to REV-ERBα. Sci Rep. 2024 Apr 10;14(1):8401. doi: 10.1038/s41598-024-58945-4. PMID: 38600172; PMCID: PMC11006950. 5: Cvammen W, Kemp MG. The REV-ERB antagonist SR8278 modulates keratinocyte viability in response to UVA and UVB radiation. Photochem Photobiol. 2024 Mar 8. doi: 10.1111/php.13930. Epub ahead of print. PMID: 38459721. 6: Shim DW, Eo JC, Kim S, Hwang I, Nam B, Shin JE, Han SH, Yu JW. Deficiency of circadian clock gene Bmal1 exacerbates noncanonical inflammasome-mediated pyroptosis and lethality via Rev-erbα-C/EBPβ-SAA1 axis. Exp Mol Med. 2024 Feb;56(2):370-382. doi: 10.1038/s12276-024-01162-w. Epub 2024 Feb 1. PMID: 38297162; PMCID: PMC10907614. 7: Baburski AZ, Becin AP, Travicic DZ, Medar MLJ, Andric SA, Kostic TS. REVERBA couples the circadian clock to Leydig cell steroidogenesis. Biofactors. 2024 Jul-Aug;50(4):738-749. doi: 10.1002/biof.2035. Epub 2023 Dec 26. PMID: 38147453. 8: Zhao S, Zhu Y, Liu H, He X, Xie J. System analysis based on the pyroptosis- related genes identifes GSDMD as a novel therapy target for skin cutaneous melanoma. J Transl Med. 2023 Nov 10;21(1):801. doi: 10.1186/s12967-023-04513-9. PMID: 37950289; PMCID: PMC10636830. 9: Chu SJ, Liao WI, Pao HP, Wu SY, Tang SE. Targeting Rev-Erbα to protect against ischemia-reperfusion-induced acute lung injury in rats. Respir Res. 2023 Oct 12;24(1):247. doi: 10.1186/s12931-023-02547-7. PMID: 37828537; PMCID: PMC10571317. 10: Kirchner SJ, Lei V, Kim PT, Patel M, Shannon JL, Corcoran D, Hughes D, Waters DK, Dzirasa K, Erdmann D, Coers J, MacLeod AS, Zhang JY. An aging- susceptible circadian rhythm controls cutaneous antiviral immunity. JCI Insight. 2023 Oct 23;8(20):e171548. doi: 10.1172/jci.insight.171548. PMID: 37725438; PMCID: PMC10619492. 11: Li C, Yang D, Yang W, Wang Y, Li D, Li Y, Xiao B, Zhang H, Zhao H, Dong H, Zhang J, Chu G, Wang A, Jin Y, Liu Y, Chen H. Hypoxia activation attenuates progesterone synthesis in goat trophoblast cells via NR1D1 inhibition of StAR expression†. Biol Reprod. 2023 Nov 15;109(5):720-735. doi: 10.1093/biolre/ioad094. PMID: 37552055. 12: Saiz N, Herrera-Castillo L, Gómez-Boronat M, Delgado MJ, Isorna E, de Pedro N. Daily rhythms of REV-ERBα and its role as transcriptional repressor of clock genes in fish hepatic oscillator. Comp Biochem Physiol A Mol Integr Physiol. 2023 Sep;283:111458. doi: 10.1016/j.cbpa.2023.111458. Epub 2023 Jun 7. PMID: 37290737. 13: Prasad C, Hahn K, Duraisamy SK, Salathe MA, Huang SK, Burris TP, Sundar IK. Rev-erbα agonists suppresses TGFβ1-induced fibroblast-to-myofibroblast transition and pro-fibrotic phenotype in human lung fibroblasts. Biochem Biophys Res Commun. 2023 Aug 20;669:120-127. doi: 10.1016/j.bbrc.2023.05.092. Epub 2023 May 24. PMID: 37269594; PMCID: PMC11034855. 14: Guo L, Cen H, Weng J, He Y, Guo X, He D, Liu K, Duan S, Yang J, Zhang X, Qin Z, Wan Y, Chen Z, Wu B. PER2 integrates circadian disruption and pituitary tumorigenesis. Theranostics. 2023 Apr 29;13(8):2657-2672. doi: 10.7150/thno.82995. PMID: 37215573; PMCID: PMC10196825. 15: Kirchner S, Lei V, Kim P, Patel M, Shannon J, Corcoran D, Hughes D, Waters D, Dzirasa K, Erdmann D, Coers J, MacLeod A, Zhang JY. An Aging-Susceptible Circadian Rhythm Controls Cutaneous Antiviral Immunity. bioRxiv [Preprint]. 2023 Apr 18:2023.04.14.536934. doi: 10.1101/2023.04.14.536934. Update in: JCI Insight. 2023 Oct 23;8(20):e171548. doi: 10.1172/jci.insight.171548. PMID: 37131751; PMCID: PMC10153172. 16: Liu G, Sun Q, Wu X, Liu Y, Chen Y, Cao Z, Hu Y, Xia H. Clock genes are expressed in cementum and regulate the proliferation and mineralization of cementoblasts. In Vitro Cell Dev Biol Anim. 2023 Jan;59(1):76-84. doi: 10.1007/s11626-023-00748-4. Epub 2023 Feb 15. PMID: 36790692. 17: Yang Y, Yang T, Zhao Z, Zhang H, Yuan P, Wang G, Zhao Z, An J, Lyu Z, Xing J, Li J. Down-regulation of BMAL1 by MiR-494-3p Promotes Hepatocellular Carcinoma Growth and Metastasis by Increasing GPAM-mediated Lipid Biosynthesis. Int J Biol Sci. 2022 Oct 18;18(16):6129-6144. doi: 10.7150/ijbs.74951. PMID: 36439870; PMCID: PMC9682529. 18: Mortimer T. Getting the clock back on its feet: targeting the circadian clock to treat osteoarthritis. FEBS J. 2022 Nov;289(21):6640-6642. doi: 10.1111/febs.16648. Epub 2022 Oct 21. PMID: 36271686. 19: Jang DY, Yang B, You MJ, Rim C, Kim HJ, Sung S, Kwon MS. Fluoxetine Decreases Phagocytic Function via REV-ERBα in Microglia. Neurochem Res. 2023 Jan;48(1):196-209. doi: 10.1007/s11064-022-03733-7. Epub 2022 Sep 1. PMID: 36048349. 20: He T, Pang S, Wang H, Yun H, Hao X, Jia L, Liu H, Wang D, Wang D, Xu H, Jie Q, Yang L, Zheng C. Drugging the circadian clock feedback cycle to ameliorate cartilage degeneration. FEBS J. 2022 Nov;289(21):6643-6658. doi: 10.1111/febs.16601. Epub 2022 Sep 1. PMID: 35997219.