[5-oxido-4-(thiophene-2-carbonyl)-1,2,5-oxadiazol-5-ium-3-yl]-thiophen-2-ylmethanone
- CAS号:7733-96-2
- 英文名:[5-oxido-4-(thiophene-2-carbonyl)-1,2,5-oxadiazol-5-ium-3-yl]-thiophen-2-ylmethanone
- 中文名:[5-oxido-4-(thiophene-2-carbonyl)-1,2,5-oxadiazol-5-ium-3-yl]-thiophen-2-ylmethanone
- CBNumber:CB34581986
- 分子式:C12H6N2O4S2
- 分子量:306.32
- MOL File:7733-96-2.mol
- 熔点 :113-114 °C(Solv: heptane (142-82-5))
- 沸点 :572.1±60.0 °C(Predicted)
- 密度 :1.67±0.1 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :DMSO:150.0(Max Conc. mg/mL);489.7(Max Conc. mM)
- 形态 :Solid
- 酸度系数(pKa) :-4.77±0.10(Predicted)
- 颜色 :White to off-white
- 海关编码 :2934999090
[5-oxido-4-(thiophene-2-carbonyl)-1,2,5-oxadiazol-5-ium-3-yl]-thiophen-2-ylmethanone性质、用途与生产工艺
- 生物活性 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 µM。
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靶点
CatSper
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体外研究
HC-056456 similarly slows the rise of [Ca 2+ ] 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 Ca 2+ 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 µM HC-056456 (estimated IC 50 near 15 µM). 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 µM HC-056456 results in partial blockade of this current. For HC-056456 action on KSper an IC 50 near 40 µM is estimated.
- 更新日期:2024/04/30
- 产品编号:HY-112729
- 产品名称:HC-056456
- CAS编号:
- 包装:1 mg
- 价格:304元
- 更新日期:2024/04/30
- 产品编号:HY-112729
- 产品名称:[5-oxido-4-(thiophene-2-carbonyl)-1,2,5-oxadiazol-5-ium-3-yl]-thiophen-2-ylmethanone HC-056456
- CAS编号:7733-96-2
- 包装:5mg
- 价格:900元
- 公司名称:TargetMol Chemicals Inc.
- 联系电话:+1-781-999-5354
- 电子邮件:support@targetmol.com
- 国家:美国
- 产品数:19973
- 优势度:58
- 公司名称:MedChemExpress
- 联系电话:--
- 电子邮件:sales@medchemexpress.com
- 国家:美国
- 产品数:6398
- 优势度:58