| Identification | Back Directory | [Name]
TD-0212 | [CAS]
1073549-10-6 | [Synonyms]
TD-0212
[1,1'-Biphenyl]-2-carboxylic acid, 4'-[[2-ethoxy-4-ethyl-5-[[[(2S)-2-mercapto-4-methyl-1-oxopentyl]amino]methyl]-1H-imidazol-1-yl]methyl]-3'-fluoro- | [Molecular Formula]
C28H34FN3O4S | [MDL Number]
MFCD31813766 | [MOL File]
1073549-10-6.mol | [Molecular Weight]
527.65 |
| Hazard Information | Back Directory | [Description]
TD-0212 is a potent, selective and orally active, dual AT1 antagonist/NEP inhibitor (ARNI) with At1 pKi-8.9 and NEP pIC50 = 9.2. TD-0212 produced blood pressure reductions similar to omapatrilat and combinations of AT1 receptor antagonists and NEP inhibitors. TD-0212 therefore provides the enhanced activity of dual AT1/NEP inhibition with a potentially lower risk of angioedema relative to dual ACE/NEP inhibition | [Uses]
TD-0212 (compound 35) is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP[1]. | [in vivo]
TD-0212 (compound 35) produces blood pressure reductions similar to omapatrilat and combinations of AT1 receptor antagonists and NEP inhibitors in models of renin-dependent and –independent hypertension[1]. | [References]
[1] McKinnell RM, et al. Discovery of TD-0212, an Orally Active Dual Pharmacology AT1 Antagonist and Neprilysin Inhibitor (ARNI). ACS Med Chem Lett. 2018 Dec 3;10(1):86-91. DOI:10.1021/acsmedchemlett.8b00462 |
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