Bioactivity | Transthyretin-IN-3 (compound 6) is a designed benzofuran analogue. Transthyretin-IN-3 selectively binds to plasma transthyretin(TTR) to inhibit Amyloid aggregation(IC50 = 5.0 ± 0.2 μM). Transthyretin-IN-3 can bind to TTR's thyroxine binding site specifically by carrying chlorine substituents at specific locations in its structure. This binding can prevent TTR tetramers from dissociating into unstable monomers[1]. |
In Vivo | Transthyretin-IN-3 ( 0.1 mg/kg, iv; 0.1 mg/kg, po; 8 h) 的口服生物利用度 (BA) 为 66.8 %,与目前的有效治疗药物效果相当[1]。Pharmacokinetic Analysis in SD rats[1]药代动力学分析[1]Route |
CAS | 3008535-20-1 |
Formula | C17H11ClI2O3 |
Molar Mass | 552.53 |
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]. Mizuguchi, Mineyuki, et al. "Development of Benziodarone Analogues with Enhanced Potency for Selective Binding to Transthyretin in Human Plasma." Journal of Medicinal Chemistry (2024). |