SR8278

SR8278
Identifiers
	IUPAC name ethyl 2-(5-methylsulfanylthiophene-2-carbonyl)-3,4-dihydro-1H-isoquinoline-3-carboxylate;
CAS Number	1254944-66-5;
PubChem CID	53393127;
ChemSpider	28189717;
CompTox Dashboard (EPA)	DTXSID80693813 ;
Chemical and physical data
Formula	C18H19NO3S2
Molar mass	361.47 g·mol−1
3D model (JSmol)	Interactive image;
	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;

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]

References

↑ 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.
↑ 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.
↑ 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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[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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See also

References