HC-056456

Modify Date: 2024-01-05 08:32:58

HC-056456 Structure
HC-056456 structure
Common Name HC-056456
CAS Number 7733-96-2 Molecular Weight 306.31700
Density N/A Boiling Point N/A
Molecular Formula C12H6N2O4S2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of HC-056456


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).

 Names

Name [5-oxido-4-(thiophene-2-carbonyl)-1,2,5-oxadiazol-5-ium-3-yl]-thiophen-2-ylmethanone
Synonym More Synonyms

 HC-056456 Biological Activity

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

[1]. Carlson AE, et al. Pharmacological targeting of native CatSper channels reveals a required role in maintenance of sperm hyperactivation. PLoS One. 2009 Aug 31;4(8):e6844.

 Chemical & Physical Properties

Molecular Formula C12H6N2O4S2
Molecular Weight 306.31700
Exact Mass 305.97700
PSA 142.11000
LogP 2.68810
Storage condition 2-8℃

 Synthetic Route

~57%

HC-056456 Structure

HC-056456

CAS#: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 & DownStream

Precursor  1

DownStream  0

 Synonyms

3,4-Bis<2-thienylcarbonyl>furazan-oxid