1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel
  3. HC-056456

HC-056456  (Synonyms: 3,4-Bis(2-thienoyl)-1,2,5-oxadiazole-N-oxide)

Cat. No.: HY-112729 Purity: 98.89%
SDS COA Handling Instructions

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).

For research use only. We do not sell to patients.

HC-056456 Chemical Structure

HC-056456 Chemical Structure

CAS No. : 7733-96-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 88 In-stock
Solution
10 mM * 1 mL in DMSO USD 88 In-stock
Solid
5 mg USD 80 In-stock
10 mg USD 120 In-stock
25 mg USD 220 In-stock
50 mg USD 350 In-stock
100 mg USD 580 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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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).

IC50 & 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

306.32

Formula

C12H6N2O4S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

[O-][N+]1=C(C(C2=CC=CS2)=O)C(C(C3=CC=CS3)=O)=NO1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (408.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2646 mL 16.3228 mL 32.6456 mL
5 mM 0.6529 mL 3.2646 mL 6.5291 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (6.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (6.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.89%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2646 mL 16.3228 mL 32.6456 mL 81.6140 mL
5 mM 0.6529 mL 3.2646 mL 6.5291 mL 16.3228 mL
10 mM 0.3265 mL 1.6323 mL 3.2646 mL 8.1614 mL
15 mM 0.2176 mL 1.0882 mL 2.1764 mL 5.4409 mL
20 mM 0.1632 mL 0.8161 mL 1.6323 mL 4.0807 mL
25 mM 0.1306 mL 0.6529 mL 1.3058 mL 3.2646 mL
30 mM 0.1088 mL 0.5441 mL 1.0882 mL 2.7205 mL
40 mM 0.0816 mL 0.4081 mL 0.8161 mL 2.0403 mL
50 mM 0.0653 mL 0.3265 mL 0.6529 mL 1.6323 mL
60 mM 0.0544 mL 0.2720 mL 0.5441 mL 1.3602 mL
80 mM 0.0408 mL 0.2040 mL 0.4081 mL 1.0202 mL
100 mM 0.0326 mL 0.1632 mL 0.3265 mL 0.8161 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HC-056456
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HY-112729
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