7733-96-2
7733-96-2 structure
- Name: HC-056456
- Chemical Name: [5-oxido-4-(thiophene-2-carbonyl)-1,2,5-oxadiazol-5-ium-3-yl]-thiophen-2-ylmethanone
- CAS Number: 7733-96-2
- Molecular Formula: C12H6N2O4S2
- Molecular Weight: 306.31700
- Catalog: Research Areas Others
- Create Date: 2017-11-22 02:02:44
- Modify Date: 2024-01-05 08:32:58
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HC-056456 is an effective but not perfectly-selective blocker of CatSper channels. The [Na+]i rise is slowed by HC-056456 (IC50~3 µM).
| Name | [5-oxido-4-(thiophene-2-carbonyl)-1,2,5-oxadiazol-5-ium-3-yl]-thiophen-2-ylmethanone |
|---|---|
| Synonyms | 3,4-Bis<2-thienylcarbonyl>furazan-oxid |
| Description | HC-056456 is an effective but not perfectly-selective blocker of CatSper channels. The [Na+]i rise is slowed by HC-056456 (IC50~3 µM). |
|---|---|
| Related Catalog | |
| Target |
CatSper[1] |
| 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 µM HC-056456 (estimated IC50 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 IC50 near 40 µM is estimated[1]. |
| References |
| Molecular Formula | C12H6N2O4S2 |
|---|---|
| Molecular Weight | 306.31700 |
| Exact Mass | 305.97700 |
| PSA | 142.11000 |
| LogP | 2.68810 |
| Storage condition | 2-8℃ |
|
~57%
7733-96-2 |
| Literature: Espenbetov, A. A.; Struchkov, Yu. T.; Churkin, Yu. D.; Panfilova, L. V. J. Gen. Chem. USSR (Engl. Transl.), 1985 , vol. 55, # 7 p. 1565 - 1570,1392 - 1396 |
| Precursor 1 | |
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| DownStream 0 | |