TD-0212 TFA

Names

[ Name ]:
TD-0212 TFA

Biological Activity

[Description]:

TD-0212 TFA 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].

[Related Catalog]:

Research Areas >> Inflammation/Immunology

Signaling Pathways >> GPCR/G Protein >> Angiotensin Receptor

Signaling Pathways >> Metabolic Enzyme/Protease >> Neprilysin

[Target]

pKi: 8.9 (AT1) .pIC50: 9.2 (NEP)[1].

[In Vitro]

TD-0212 provides the enhanced activity of dual AT1/NEP inhibition with a potentially lower risk of angioedema relative to dual ACE/NEP inhibition[1].

[In Vivo]

TD-0212 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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₀H₃₅F₄N₃O₆S

[ Molecular Weight ]:
641.67

TD-0212 TFA

Names

Biological Activity

Chemical & Physical Properties

Related Compounds