Bioactivity | BA6b9 is an allosteric inhibitor of SK4 channels that targets the CaM–PIP2-binding domain with a IC50 value of 8.6 µM (WT SK4). BA6b9 inhibits SK4 channels by interacting with two specific residues, Arg191 and His192 in the S4–S5 linker. BA6b9 significantly prolongs atrial and atrioventricular effective refractory period (ERP) and reduces atrial fibrillation (AF) induction in rat isolated hearts, which has the potential to be used for the research of arrhythmia [1]. |
Target | IC50: 8.6 μM (WT SK4 Channel) |
Invitro | BA6b9 (10 μM) 通过将 Ca2+ 激活的 EC50 从 65 nM 提高到 435 nM 来强烈抑制 Ca2+ 激活的 SK4 通道[1]。BA6b9 (10 μM) 可以在成年雄性 Sprague-Dawley 大鼠 Langendorff 分离心脏模型 (200-250 g) 中导致心率降低、PR 间期延长、心房和房室结有效不应期 (ERP) 延长,并抑制卡巴胆碱诱导的心房颤动 (AF) [1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> BA6b9 相关抗体: |
CAS | 609335-29-7 |
Formula | C14H19NO2 |
Molar Mass | 233.31 |
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]. Shira Burg, et al. Allosteric inhibitors targeting the calmodulin-PIP2 interface of SK4 K+ channels for atrial fibrillation treatment. Proc Natl Acad Sci U S A. 2022 Aug 23;119(34):e2202926119. |