Drug Information

Drug General Information
Drug ID
D0YS1U
Former ID
DIB018038
Drug Name
sparsentan
Synonyms
RE-021; retrophin; DARA-a (Dual Acting Receptor Antagonist of angiotension and endothelin receptors); compound 7 [PMID 15634011]
Drug Type
Small molecular drug
Indication Myocardial infarction [ICD9: 410; ICD10:I21, I22] Phase 2 [527366]
Formula
C32H40N4O5S
InChI
InChI=1S/C32H40N4O5S/c1-5-7-14-29-33-32(17-10-11-18-32)31(37)36(29)20-24-15-16-26(25(19-24)21-40-6-2)27-12-8-9-13-28(27)42(38,39)35-30-22(3)23(4)41-34-30/h8-9,12-13,15-16,19H,5-7,10-11,14,17-18,20-21H2,1-4H3,(H,34,35)
InChIKey
WRFHGDPIDHPWIQ-UHFFFAOYSA-N
PubChem Compound ID
10257882
PubChem Substance ID
15261283, 22639359, 41243131, 75635872, 85229343, 103441000, 104061216, 129622448, 134338955, 140307738, 163642156, 198948890, 224747591, 226845654, 252166658
Target and Pathway
Target(s) Type-1 angiotensin II receptor Target Info Antagonist [527799]
Endothelin-1 receptor Target Info Antagonist [527799]
KEGG Pathway Calcium signaling pathway
cGMP-PKG signaling pathway
Neuroactive ligand-receptor interaction
Adrenergic signaling in cardiomyocytes
Vascular smooth muscle contraction
Renin-angiotensin system
Renin secretion
Pathways in cancerhsa04020:Calcium signaling pathway
cAMP signaling pathway
Pathways in cancer
NetPath Pathway TGF_beta_Receptor Signaling PathwayNetPath_16:IL4 Signaling Pathway
PANTHER Pathway Angiotensin II-stimulated signaling through G proteins and beta-arrestinP00019:Endothelin signaling pathway
Pathway Interaction Database Arf6 trafficking events
Arf6 signaling events
Angiopoietin receptor Tie2-mediated signalingendothelinpathway:Endothelins
EGFR-dependent Endothelin signaling events
PathWhiz Pathway Angiotensin Metabolism
Muscle/Heart Contraction
Reactome Peptide ligand-binding receptors
G alpha (q) signalling eventsR-HSA-375276:Peptide ligand-binding receptors
G alpha (q) signalling events
WikiPathways ACE Inhibitor Pathway
GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
Peptide GPCRs
Allograft Rejection
GPCR ligand binding
GPCR downstream signalingWP98:Prostaglandin Synthesis and Regulation
Endothelin Pathways
GPCR downstream signaling
GPCRs, Other
References
Ref 527366Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. J Med Chem. 2005 Jan 13;48(1):171-9.
Ref 527799J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.

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