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HC-056456

CAS No. : 7733-96-2

MCE 站：HC-056456

产品活性：HC-056456 是一种有效但不完全选择性的 CatSper 通道阻断剂。HC-056456 减慢 [Na⁺]_i 上升，IC₅₀ 为 3 ?M。

研究领域：Others

作用靶点：Others

In Vitro: HC-056456 similarly slows the rise of [Ca²⁺]_i that is evoked by alkaline depolarization and reported by fura-2. HC-056456 also selectively and reversibly decreased CatSper currents recorded from patch-clamped sperm. HC-056456 produces a pharmacological phenocopy of the CatSper-null sperm. Acute application of HC-056456 causes rapid loss of flagellar waveform asymmetry from hyperactivated sperm, indicating that continued entry of Ca²⁺ through CatSper channels is required to maintain hyperactivation. HC-056456 selectively and reversibly blocks CatSper currents. The specificity and reversibility of the blockade of CatSper-dependent currents by HC-056456 is examined by using patch clamp recordings. The observed current is blocked slightly more than 50% by 20 ?M HC-056456 (estimated IC₅₀ near 15 ?M). In concept, it remains possible that CatSper channel heterogeneity explains residual HC-056456-resistant current. The action of HC-056456 on KSper channels, the other major cation channel observed in patch-clamped sperm, is also examined. Subsequent application of 50 ?M HC-056456 results in partial blockade of this current. For HC-056456 action on KSper an IC₅₀ near 40 ?M is estimated.

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