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TD-0212

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

M.Wt 527.655
Formula C28H34FN3O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(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

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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