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).
Product information
CAS Number: 7733-96-2
Molecular Weight: 306.32
Formula: C12H6N2O4S2
Chemical Name: bis(thiophene-2-carbonyl)-1,2,5-oxadiazol-2-ium-2-olate
Smiles: [O-][N+]1ON=C(C=1C(=O)C1=CC=CS1)C(=O)C1=CC=CS1
InChiKey: RUQGCDMXFBOTMW-UHFFFAOYSA-N
InChi: InChI=1S/C12H6N2O4S2/c15-11(7-3-1-5-19-7)9-10(14(17)18-13-9)12(16)8-4-2-6-20-8/h1-6H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 150 mg/mL (489.68 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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