827034-92-4
Chemical Structure
NA808
- CAS No.: 827034-92-4
- Formula:C35H49NO10
- Molecular Weight:643.76
IUPAC Name: (S)-2-((S,E)-1-(((S)-2-(4-(but-2-yn-1-yloxy)phenyl)-1-carboxyethyl)amino)-1,11-dioxooctadec-3-en-2-yl)-2-hydroxysuccinic acid
InChIKey: RZHKGHCZVMTIDL-XSRFUOEWSA-N
SMILES: OC(C[C@](C(O)=O)(O)[C@H](/C=C/CCCCCCC(CCCCCCC)=O)C(N[C@H](C(O)=O)CC1=CC=C(C=C1)OCC#CC)=O)=O
Biological Activity: NA808 is an Serine Palmitoyltransferase (SPT) inhibitor. NA808 reduces sphingomyelin synthesis, inhibits its activation in hepatic stellate cells, and decreases the expression of α-SMA protein and mRNA, as well as collagen 1A1 mRNA (IC50 0.16, 0.12, and 0.11 μM, respectively). NA808 inhibits HCV replication and reduces NS3 and RdRp protein expression in HCV replicon cells without significant cytotoxicity and exhibits almost no immunosuppressive effect at effective concentrations. NA808 demonstrates broad-spectrum antiviral activity in humanized chimeric liver mice infected with various HCV genotypes, and dose-dependently reduces serum and hepatic HCV RNA levels. NA808 can be used for research on non-alcoholic steatohepatitis and hepatitis C virus infection[1][2][3][4].
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NA808 | NA808 is an Serine Palmitoyltransferase (SPT) inhibitor. NA808 reduces sphingomyelin synthesis, inhibits its activation in hepatic stellate cells, and decreases the expression of α-SMA protein and mRNA, as well as collagen 1A1 mRNA (IC50 0.16, 0.12, and 0.11 μM, respectively). NA808 inhibits HCV replication and reduces NS3 and RdRp protein expression in HCV replicon cells without significant cytotoxicity and exhibits almost no immunosuppressive effect at effective concentrations. NA808 demonstrates broad-spectrum antiviral activity in humanized chimeric liver mice infected with various HCV genotypes, and dose-dependently reduces serum and hepatic HCV RNA levels. NA808 can be used for research on non-alcoholic steatohepatitis and hepatitis C virus infection. | |||||||||||||||||||||
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- [1]. Hada N, et al. Novel oral SPT inhibitor CH5169356 inhibits hepatic stellate cell activation and ameliorates hepatic fibrosis in mouse models of non-alcoholic steatohepatitis (NASH). Pharmacol Res Perspect. 2023 Jun;11(3):e01094. [Content Brief]
- [2]. Yamane M, et al. Evaluation of the non-linearity of NA808 in liver not reflected in plasma using a rat pharmacokinetic study and PBPK modelling. Xenobiotica. 2023 Dec;53(6-7):498-506. [Content Brief]
- [3]. Katsume A, et al. A serine palmitoyltransferase inhibitor blocks hepatitis C virus replication in human hepatocytes. Gastroenterology. 2013 Oct;145(4):865-73. [Content Brief]
- [4]. Hirata Y, et al. Self-enhancement of hepatitis C virus replication by promotion of specific sphingolipid biosynthesis. PLoS Pathog. 2012;8(8):e1002860. [Content Brief]
Keywords
