| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
CatSper (cation channel of sperm) calcium channels.
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|---|---|
| ln Vitro |
Similar to fura-2, HC-056456 reduced the rise in [Ca2+]i caused by flat ground depotentiation. Reversibly and selectively lowering CatSper current captured via the patch-clamp button is another feature of HC-056456. A CatSper-null pharmacological phenotype is produced by HC-056456. The hyperactivated agent rapidly loses its hairy evaporability upon acute administration of HC-056456, suggesting that continuous Ca2+ input via CatSper channels is required to keep the hyperactivated agent active. CatSper current is selectively and reversibly boiled by HC-056456. Utilizing patch-clamp recordings, investigate the reversibility and intermittency of CatSper-dependent current flow by HC-056456. Twenty μM HC-056456 inhibited about half of the observed current (the calculated IC50 is closer to 15 μM). Theoretically, the remaining HC-056456-resistant current could still be explained by CatSper channel heterogeneity. It was also investigated how HC-056456 affected KSper channels, which are the other main cation channel seen in the membrane clamp. A subsequent application of 50 μM HC-056456 caused this current to be partially blocked. The calculated IC50 for HC-056456's impact on KSper is near 40 μM [1].
HC-056456 slows the rise of intracellular sodium [Na+]i with an IC50 of 3 µM. It is a CatSper channel blocker that inhibits calcium influx in sperm, thereby affecting sperm motility and capacitation. The compound is effective but not perfectly selective, meaning it may have off-target effects at higher concentrations. |
| ln Vivo |
In vivo, HC-056456 has been studied for its effects on male fertility. As a CatSper channel blocker, it inhibits sperm motility and fertilization in animal models. The compound has potential as a non-hormonal male contraceptive. Specific dosing regimens and detailed efficacy data are available in preclinical literature.
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| Enzyme Assay |
CatSper channel activity is assessed using patch-clamp electrophysiology on sperm cells or cells expressing recombinant CatSper channels. Calcium influx is measured using fluorescent calcium indicators such as Fluo-4. Sodium influx is measured using sodium-sensitive dyes. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cellular activity is evaluated in sperm cells isolated from mammals. Sperm are treated with HC-056456 at various concentrations and sperm motility, hyperactivation, and acrosome reaction are assessed using computer-assisted sperm analysis (CASA). Intracellular calcium and sodium levels are measured using fluorescent indicators.
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| Animal Protocol |
In vivo efficacy is studied in male animal models. HC-056456 is administered orally or via intraperitoneal injection. Sperm motility and fertility are assessed by mating studies or in vitro fertilization assays. Testicular and epididymal sperm counts and morphology are evaluated. The compound is investigated for male contraceptive potential.
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| ADME/Pharmacokinetics |
HC-056456 has a molecular formula of C12H6N2O4S2 and molecular weight of 306.32. Purity is typically >98% by HPLC. The compound is soluble in DMSO (≥150 mg/mL). Detailed pharmacokinetic parameters including half-life, oral bioavailability, and plasma protein binding are not extensively characterized in publicly available literature.
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| Toxicity/Toxicokinetics |
Safety data for HC-056456 indicate it is a research compound for laboratory use only. Specific toxicological profiles including acute toxicity, organ toxicity, and genotoxicity are not extensively published. As a CatSper inhibitor, it may affect male fertility. Standard laboratory safety practices should be followed during handling.
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| References | |
| Additional Infomation |
HC-056456 is a research tool compound for studying CatSper channel function and male fertility. It is not approved for clinical use. The compound has been investigated as a potential non-hormonal male contraceptive due to its ability to inhibit sperm motility and fertilization by blocking CatSper calcium channels.
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| Molecular Formula |
C12H6N2O4S2
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|---|---|
| Molecular Weight |
306.31
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| Exact Mass |
305.977
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| CAS # |
7733-96-2
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| PubChem CID |
573747
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| Appearance |
White to off-white solid powder
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| LogP |
2.688
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
409
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RUQGCDMXFBOTMW-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
[5-oxido-4-(thiophene-2-carbonyl)-1,2,5-oxadiazol-5-ium-3-yl]-thiophen-2-ylmethanone
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| Synonyms |
HC056456; HC 056456; HC-056456
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~408.07 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2647 mL | 16.3233 mL | 32.6467 mL | |
| 5 mM | 0.6529 mL | 3.2647 mL | 6.5293 mL | |
| 10 mM | 0.3265 mL | 1.6323 mL | 3.2647 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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