| Bioactivity | I1421 is an activator of the cystic fibrosis transmembrane conductance regulator (CFTR) with an EC50 of 64 nM for WT CFTR currents. I1421 also allosterically activates multiple mutants causing cystic fibrosis (CF) with good in vivo potency, with an oral bioavailability of 60% in mice corresponding to a half-life of 75 min. I1421 synergizes with Elexacaftor (HY-111772) to enhance CFTR currents[1]. |
| Target | EC50: 64 nM (WT CFTR) |
| In Vivo | I1421 (10 mg/kg; ip, po, sc; 单剂量) 在 C57BL/6 小鼠中的吸收速率快，进行 3 种不同给药方式后，腹膜内和口服给药后 15 min 观察到的最大血浆浓度 (Cmax) 分别为 7.4 μM 和 3.4 μM，同时腹膜内给药后的血浆水平高于其他两种给药途径[1]。I1421 (3 mg/kg; iv, po; 单剂量) 在进行口服和静脉注射的小鼠中，生物利用度为 60%，但口服 T1/2 较短（75 min）[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
| Formula | C18H18FN3O3 |
| Molar Mass | 343.35 |
| 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]. Liu F, et al. Structure-based discovery of CFTR potentiators and inhibitors. Cell. 2024 May 23:S0092-8674(24)00472-0. |