General Information of Drug (ID: DM7OVMH)

Drug Name
OPC-21268 Drug Info
Synonyms
Acetamide, N-(3-(4-((4-(3,4-dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl)carbonyl)phenoxy)propyl)-; Opc 21268; 131631-89-5; Fuscoside; 1-(1-(4-(3-Acetylaminopropoxy)benzoyl)-4-piperidyl)-3,4-dihydro-2(1H)-quinolinone; CHEMBL296908; OPC-1268; N-[3-[4-[4-(2-oxo-3,4-dihydroquinolin-1-yl)piperidine-1-carbonyl]phenoxy]propyl]acetamide; N-(3-(4-(4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidine-1-carbonyl)phenoxy)propyl)acetamide; ACMC-20mu6h; AC1L3G6H; SCHEMBL3504368; GTPL2196; CTK0H6673; EX-A593
Indication
Disease Entry ICD 11 Status REF
Cardiac disease BA00-BE2Z Discontinued in Phase 2 [1]
Cross-matching ID
PubChem CID
114904
CAS Number
CAS 131631-89-5
TTD Drug ID
DM7OVMH

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Arachidonate 5-lipoxygenase (5-LOX) TT2J34L LOX5_HUMAN Inhibitor [2]
Vasopressin V1 receptor (V1R) TTPFZJ1 NOUNIPROTAC Antagonist [3]
Vasopressin V1a receptor (V1AR) TT4TFGN V1AR_HUMAN Antagonist [4]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Vasopressin V1a receptor (V1AR) DTT AVPR1A 4.689 3.609 4.591 3.878
Arachidonate 5-lipoxygenase (5-LOX) DTT ALOX5 4.966 5.133 5.358 6.128
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 Cardiac disease
ICD Disease Classification BA00-BE2Z
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Arachidonate 5-lipoxygenase (5-LOX) DTT ALOX5 4.15E-01 -0.06 -0.15
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: 2196).
2 Fuscoside: an anti-inflammatory marine natural product which selectively inhibits 5-lipoxygenase. Part II: Biochemical studies in the human neutrophil. J Pharmacol Exp Ther. 1992 Aug;262(2):874-82.
3 Vasopressin (ADH). Nippon Rinsho. 1992 Dec;50(12):2893-900.
4 Nonpeptide vasopressin receptor antagonists: development of selective and orally active V1a, V2 and V1b receptor ligands. Prog Brain Res. 2002;139:197-210.