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1073549-11-7

1073549-11-7 structure
1073549-11-7 structure
  • Name: TD-0212 TFA
  • Chemical Name: TD-0212 TFA
  • CAS Number: 1073549-11-7
  • Molecular Formula: C30H35F4N3O6S
  • Molecular Weight: 641.67
  • Catalog: Signaling Pathways GPCR/G Protein Angiotensin Receptor
  • Create Date: 2020-01-23 19:04:51
  • Modify Date: 2024-01-12 17:59:34
  • 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].

Name TD-0212 TFA
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
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.

Molecular Formula C30H35F4N3O6S
Molecular Weight 641.67