| Bioactivity | 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]. |
| Target | pKi: 8.9 (AT1)pIC50: 9.2 (NEP). |
| Invitro | TD-0212 (compound 35) 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 (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]. |
| Name | TD-0212 |
| CAS | 1073549-10-6 |
| Formula | C28H34FN3O4S |
| Molar Mass | 527.65 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |