HC-056456 (3,4-Bis(2-thienoyl)-1,2,5-oxadiazole-N-oxide) (Synonyms: 3,4-Bis(2-thienoyl)-1,2,5-oxadiazole-N-oxide) |
Catalog No.GC30574
One-Click Copy Product Info
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HC-056456 (3,4-Bis(2-thiénoyl)-1,2,5-oxadiazole-N-oxyde) est un bloqueur efficace mais pas parfaitement sélectif des canaux CatSper.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 7733-96-2
Sample solution is provided at 25 µL, 10mM.
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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).
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].
[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.
| Cas No. | 7733-96-2 | SDF | |
| Synonymes | 3,4-Bis(2-thienoyl)-1,2,5-oxadiazole-N-oxide | ||
| Canonical SMILES | [O-][N+]1=C(C(C2=CC=CS2)=O)C(C(C3=CC=CS3)=O)=NO1 | ||
| Formula | C12H6N2O4S2 | M.Wt | 306.32 |
| Solubility | DMSO : ≥ 150 mg/mL (489.68 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2646 mL | 16.3228 mL | 32.6456 mL |
| 5 mM | 652.9 μL | 3.2646 mL | 6.5291 mL |
| 10 mM | 326.5 μL | 1.6323 mL | 3.2646 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)