Bioactivity | VU0546110 is a selective inhibitor of the sperm-specific potassium channel SLO3, with IC50s of 1.287 μM (SLO3) and 59.80 μM (SLO1) in HEK293 cells, respectively. VU0546110 blocks heterologous SLO3 currents and endogenous K+ currents in human sperm. VU0546110 halts sperm hyperpolarization, induced acrosome reaction, and hyper-activated motility. VU0546110 has contraceptive potential[1]. |
Target | 1.287 μM (SLO3), 59.80 μM (SLO1) |
Invitro | VU0546110 (10 μM) 在细胞内游离 Ca2+ 浓度为 0-50 µM 时阻断人类精子中的 K+ 电流[1]。VU0546110 (2.5 μM) 抑制人类精子在 pH 8.0 时具有的超极化膜电位[1]。VU0546110 (2.5-10 μM) 抑制人类精子中过度激活的运动和 Ca2+ 促进剂 A23187 (HY-N6687) 或黄体酮 (HY-N0437) 诱导的顶体反应[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> VU0546110 相关抗体: |
CAS | 1421523-00-3 |
Formula | C24H31NO4S2 |
Molar Mass | 461.64 |
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]. Lyon M, et al. A selective inhibitor of the sperm-specific potassium channel SLO3 impairs human sperm function. Proceedings of the National Academy of Sciences of the United States of America. 2023, 120(4), e2212338120. |