Firsocostat

Firsocostat is an acetyl-CoA carboxylase inhibitor that functions in the liver. Its original designation was GS-0976.[1] It was discovered by Nimbus Therapeutics.[2] The drug is under development by Gilead as a treatment for non-alcoholic fatty liver disease.[3]

Firsocostat
Names
IUPAC name
2-[1-[(2R)-2-(2-methoxyphenyl)-2-(oxan-4-yloxy)ethyl]-5-methyl-6-(1,3-oxazol-2-yl)-2,4-dioxothieno[2,3-d]pyrimidin-3-yl]-2-methylpropanoic acid
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
DrugBank
KEGG
UNII
  • InChI=1S/C28H31N3O8S/c1-16-21-24(32)31(28(2,3)26(33)34)27(35)30(25(21)40-22(16)23-29-11-14-38-23)15-20(39-17-9-12-37-13-10-17)18-7-5-6-8-19(18)36-4/h5-8,11,14,17,20H,9-10,12-13,15H2,1-4H3,(H,33,34)/t20-/m0/s1
    Key: ZZWWXIBKLBMSCS-FQEVSTJZSA-N
  • CC1=C(SC2=C1C(=O)N(C(=O)N2C[C@@H](C3=CC=CC=C3OC)OC4CCOCC4)C(C)(C)C(=O)O)C5=NC=CO5
Properties
C28H31N3O8S
Molar mass 569.63 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references

References
  1. Alkhouri, Naim; Lawitz, Eric; Noureddin, Mazen; DeFronzo, Ralph; Shulman, Gerald I. (1 February 2020). "GS-0976 (Firsocostat): an investigational liver-directed acetyl-CoA carboxylase (ACC) inhibitor for the treatment of non-alcoholic steatohepatitis (NASH)". Expert Opinion on Investigational Drugs. 29 (2): 135–141. doi:10.1080/13543784.2020.1668374.
  2. Harriman, Geraldine; Greenwood, Jeremy; Bhat, Sathesh; Huang, Xinyi; Wang, Ruiying; Paul, Debamita; Tong, Liang; Saha, Asish K.; Westlin, William F.; Kapeller, Rosana; Harwood, H. James (29 March 2016). "Acetyl-CoA carboxylase inhibition by ND-630 reduces hepatic steatosis, improves insulin sensitivity, and modulates dyslipidemia in rats". Proceedings of the National Academy of Sciences. 113 (13). doi:10.1073/pnas.1520686113.
  3. Alkhouri, Naim (1 February 2020). "NASH and NAFLD: emerging drugs, therapeutic targets and translational and clinical challenges". Expert Opinion on Investigational Drugs. 29 (2): 87–87. doi:10.1080/13543784.2020.1721169.
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