1809064-23-0
Chemical Structure
PF-06427878
- CAS No.: 1809064-23-0
- Formula:C26H28N4O5
- Molecular Weight:476.52
IUPAC Name: (R)-3-((2-(3-(2-ethoxyphenoxy)piperidin-1-yl)pyrimidine-5-carboxamido)methyl)benzoic acid
InChIKey: IDVOZBCJUVAIMF-OAQYLSRUSA-N
SMILES: O=C(O)C1=CC=CC(CNC(C2=CN=C(N3C[C@H](OC4=CC=CC=C4OCC)CCC3)N=C2)=O)=C1
Biological Activity: PF-06427878 is an orally active, selective liver-targeted diacylglycerol acyltransferase 2 (DGAT2) inhibitor with IC50s of 99 nM and 202 nM for human and rat DGAT2, respectively. PF-06427878 shows greater than 470-fold selectivity for DGAT2 over DGAT1, MGAT1, MGAT2 and MGAT3. PF-06427878 can improve liver steatosis and function. PF-06427878 can be used for the study of nonalcoholic fatty liver diseases[1][2].
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PF-06427878 | PF-06427878 is an orally active, selective liver-targeted diacylglycerol acyltransferase 2 (DGAT2) inhibitor with IC50s of 99 nM and 202 nM for human and rat DGAT2, respectively. PF-06427878 shows greater than 470-fold selectivity for DGAT2 over DGAT1, MGAT1, MGAT2 and MGAT3. PF-06427878 can improve liver steatosis and function. PF-06427878 can be used for the study of nonalcoholic fatty liver diseases. | |||||||||||||||||||||
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- [1]. Amin NB, et al. Targeting diacylglycerol acyltransferase 2 for the treatment of nonalcoholic steatohepatitis. Sci Transl Med. 2019 Nov 27;11(520):eaav9701. [Content Brief]
- [2]. Sharma R, et al. Mitigating a Bioactivation Liability with an Azetidine-Based Inhibitor of Diacylglycerol Acyltransferase 2 (DGAT2) En Route to the Discovery of the Clinical Candidate Ervogastat. Chem Res Toxicol. 2023 Jun 19;36(6):934-946. [Content Brief]
Keywords
