Bioactivity | AHR antagonist 8 (compound SG-02) is a regulator of utrophin, a homolog of dystrophin, and an AhR antagonist (Kd: 41.68 nM). Studies have shown that 800 nM of AHR antagonist 8 can upregulate utrophin by 2.7 times. AHR antagonist 8 also stimulates increased MyHC expression, suggesting that it has the potential to enhance myogenesis. After ADME evaluation, AHR antagonist 8 also has a certain oral bioavailability[1]. |
Target | UtrophinKd: 41.68 nM (AHR) |
Formula | C16H14FN3O2S |
Molar Mass | 331.36 |
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]. Ghosh S, Arshi MU, Ghosh S, Jash M, Sen S, Mamchaoui K, Bhattacharyya S, Rana NK, Ghosh S. Discovery of Quinazoline and Quinoline-Based Small Molecules as Utrophin Upregulators via AhR Antagonism for the Treatment of Duchenne Muscular Dystrophy. J Med Chem. 2024 Jun 13;67(11):9260-9276. |