Chemical Structure : TD-0212
CAS No.:
1073549-10-6
TD-0212
(TD0212;TD 0212)
Catalog No.: PC-35877Not For Human Use, Lab Use Only.
TD-0212 (TD0212) is a potent, orally efficacious, dual AT1 antagonist/Neprilysin (NEP) inhibitor with pKi of 8.9 (AT1) and pIC50 of 9.2 (NEP).
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
TD-0212 (TD0212) is a potent, orally efficacious, dual AT1 antagonist/Neprilysin (NEP) inhibitor with pKi of 8.9 (AT1) and pIC50 of 9.2 (NEP); produces blood pressure reductions similar to omapatrilat and combinations of AT1 receptor antagonists and NEP inhibitors in models of renin-dependent and -independent hypertension, does not increase TPE at antihypertensive doses in rat tracheal plasma extravasation (TPE) models.
Physicochemical Properties
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M.Wt
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527.655
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Formula
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C28H34FN3O4S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20 °C 12 Months; 4°C 6 Months
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- In Solvent
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-80 °C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(S)-4'-((2-ethoxy-4-ethyl-5-((2-mercapto-4-methylpentanamido)methyl)-1H-imidazol-1-yl)methyl)-3'-fluoro-[1,1'-biphenyl]-2-carboxylic acid
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References
1. R. Murray McKinnell, et al. Discovery of TD-0212, an Orally Active Dual Pharmacology AT1 Antagonist and Neprilysin Inhibitor (ARNI). ACS Med. Chem. Lett. DOI: 10.1021/acsmedchemlett.8b00462
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