Drug Information
| Drug General Information | Top | |||
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| Drug ID |
D0R7YY
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| Former ID |
DIB015427
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| Drug Name |
Darusentan
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| Synonyms |
Endothelin antagonist, BASF; HMR-4005; LU-127043; LU-135252
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| Drug Type |
Small molecular drug
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| Indication | Hypotension [ICD-11: BA20-BA21] | Phase 3 | [1], [2] | |
| Company |
Gilead Sciences; Knoll GmbH
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| Structure |
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Download2D MOL |
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| Formula |
C22H22N2O6
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| Canonical SMILES |
COC1=CC(=NC(=N1)OC(C(=O)O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)OC
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| InChI |
1S/C22H22N2O6/c1-27-17-14-18(28-2)24-21(23-17)30-19(20(25)26)22(29-3,15-10-6-4-7-11-15)16-12-8-5-9-13-16/h4-14,19H,1-3H3,(H,25,26)/t19-/m1/s1
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| InChIKey |
FEJVSJIALLTFRP-LJQANCHMSA-N
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| CAS Number |
CAS 171714-84-4
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| PubChem Compound ID | ||||
| PubChem Substance ID |
7979815, 10258564, 12015030, 14904202, 14928792, 33500713, 49881054, 53788749, 57395363, 76344031, 103191671, 104003423, 104426232, 118855309, 126681579, 127834770, 135154690, 137249396, 139988415, 152133971, 163884607, 170466416, 175426886, 178100494, 179150062, 187071946, 198954978, 198979503, 198991928, 223661592, 227075098
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| Target and Pathway | Top | |||
|---|---|---|---|---|
| Target(s) | Endothelin A receptor (EDNRA) | Target Info | Antagonist | [3] |
| KEGG Pathway | Calcium signaling pathway | |||
| cGMP-PKG signaling pathway | ||||
| cAMP signaling pathway | ||||
| Neuroactive ligand-receptor interaction | ||||
| Vascular smooth muscle contraction | ||||
| Renin secretion | ||||
| Pathways in cancer | ||||
| NetPath Pathway | IL4 Signaling Pathway | |||
| Panther Pathway | Endothelin signaling pathway | |||
| Pathway Interaction Database | Endothelins | |||
| EGFR-dependent Endothelin signaling events | ||||
| Reactome | Peptide ligand-binding receptors | |||
| G alpha (q) signalling events | ||||
| WikiPathways | Prostaglandin Synthesis and Regulation | |||
| GPCRs, Class A Rhodopsin-like | ||||
| Gastrin-CREB signalling pathway via PKC and MAPK | ||||
| Peptide GPCRs | ||||
| Endothelin Pathways | ||||
| GPCR ligand binding | ||||
| GPCR downstream signaling | ||||
| GPCRs, Other | ||||
| References | Top | |||
|---|---|---|---|---|
| REF 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: 3508). | |||
| REF 2 | ClinicalTrials.gov (NCT00389779) DORADO-AC - Optimized Doses of Darusentan as Compared to an Active Control in Resistant Hypertension. U.S. National Institutes of Health. | |||
| REF 3 | Endothelin ETA receptor blockade with darusentan increases sodium and potassium excretion in aging rats. J Cardiovasc Pharmacol. 2006 Mar;47(3):456-62. | |||
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