General Information of Drug (ID: DM4JZPT)

Drug Name
Squalestatin 1 Drug Info
Synonyms
Zaragozic acid A; squalestatin 1; Squalestatin; 142561-96-4; ZARAGOZIC ACIDS A; UNII-1117HVX02L; CHEMBL280978; CHEBI:75170; 1117HVX02L; 1S-((4S-acetoxy-5R-methyl-3-methylene-6-phenylhexyl)-6-(E)-4S,6S-dimethyloct-2-enoyloxy)-4,7S-dihydroxy-2,8-dioxabicyclo[321]octane-3S,4S,5R-tricarboxylic acid; L-erythro-L-glycero-D-altro-7-Trideculo-7,4-furanosonic acid, 2,7-anhydro-3,4-di-C-carboxy-8,9,10,12,13-pentadeoxy-10-methylene-12-(phenylmethyl)-, 11-acetate 5-(4,6-dimethyl-2-octenoate), (5(2E,4S,6S),7S)-; Squalestatin 1, Glaxo; Zaragozic acid A, Glaxo
Indication
Disease Entry ICD 11 Status REF
Arteriosclerosis BD40 Terminated [1]
Cross-matching ID
PubChem CID
6438355
ChEBI ID
CHEBI:75170
CAS Number
CAS 142561-96-4
TTD Drug ID
DM4JZPT

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
RAC-alpha serine/threonine-protein kinase (AKT1) TTWTSCV AKT1_HUMAN Inhibitor [2]
Squalene synthetase (FDFT1) TTFQEO5 FDFT_HUMAN Modulator [3]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
RAC-alpha serine/threonine-protein kinase (AKT1) DTT AKT1 7.399 7.276 7.816 6.959
Squalene synthetase (FDFT1) DTT FDFT1 7.652 8.602 8.32 8.907
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Arteriosclerosis
ICD Disease Classification BD40
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Squalene synthetase (FDFT1) DTT FDFT1 7.85E-01 -0.09 -0.38
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3057).
2 Raft nanodomains contribute to Akt/PKB plasma membrane recruitment and activation. Nat Chem Biol. 2008 Sep;4(9):538-47.
3 Squalestatin 1, a potent inhibitor of squalene synthase, which lowers serum cholesterol in vivo. J Biol Chem. 1992 Jun 15;267(17):11705-8.