TD-0212
TD-0212 Basic information
- Product Name:
- TD-0212
- 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-
- TD0212,TD 0212
- CAS:
- 1073549-10-6
- MF:
- C28H34FN3O4S
- MW:
- 527.65
- Mol File:
- 1073549-10-6.mol
TD-0212 Usage And Synthesis
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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