SR8278

SR-8278 is an experimental drug that was developed as an antagonist of Rev-ErbAα.[1] It has been used to demonstrate potential applications of Rev-ErbAα antagonists in the treatment of conditions such as Duchenne muscular dystrophy and Alzheimer's disease.[2][3]

SR8278
Identifiers
IUPAC name
  • ethyl 2-(5-methylsulfanylthiophene-2-carbonyl)-3,4-dihydro-1H-isoquinoline-3-carboxylate
CAS Number
PubChem CID
ChemSpider
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC18H19NO3S2
Molar mass361.47 g·mol−1
3D model (JSmol)
SMILES
  • CCOC(=O)C1CC2=CC=CC=C2CN1C(=O)C3=CC=C(S3)SC
InChI
  • 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
  • Key:UIEBLUZPSFAFOC-UHFFFAOYSA-N

See also

References
  1. Kojetin D, Wang Y, Kamenecka TM, Burris TP (February 2011). "Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB". ACS Chemical Biology. 6 (2): 131–4. doi:10.1021/cb1002575. PMC 3042041. PMID 21043485.
  2. Welch RD, Billon C, Valfort AC, Burris TP, Flaveny CA (December 2017). "Pharmacological inhibition of REV-ERB stimulates differentiation, inhibits turnover and reduces fibrosis in dystrophic muscle". Scientific Reports. 7 (1): 17142. Bibcode:2017NatSR...717142W. doi:10.1038/s41598-017-17496-7. PMC 5719458. PMID 29215066.
  3. Lee J, Kim DE, Griffin P, Sheehan PW, Kim DH, Musiek ES, Yoon SY (February 2020). "Inhibition of REV-ERBs stimulates microglial amyloid-beta clearance and reduces amyloid plaque deposition in the 5XFAD mouse model of Alzheimer's disease". Aging Cell. 19 (2): e13078. doi:10.1111/acel.13078. PMC 6996949. PMID 31800167.
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