WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 531948
CAS#: 7733-96-2
Description: HC-056456 is a CatSper channel modulator.
MedKoo Cat#: 531948
Name: HC-056456
CAS#: 7733-96-2
Chemical Formula: C12H6N2O4S2
Exact Mass: 305.9769
Molecular Weight: 306.31
Elemental Analysis: C, 47.05; H, 1.97; N, 9.15; O, 20.89; S, 20.93
Synonym: HC-056456; HC 056456; HC056456.
IUPAC/Chemical Name: bis[(thiophen-2-yl)carbonyl]-1,2,5-oxadiazol-2-ium-2-olate
InChi Key: RUQGCDMXFBOTMW-UHFFFAOYSA-N
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
SMILES Code: [O-][N+]1=C(C(C2=CC=CS2)=O)C(C(C3=CC=CS3)=O)=NO1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
| Biological target: | HC-056456 is a blocker of CatSper channels. |
| In vitro activity: | N/A |
| In vivo activity: | The CatSper channel is the predominant route for evoked Ca2+ entry into intact mouse sperm. Compound HC-056456 was identified as a potential inhibitor of CatSper in a chemical-library screenThe efficacy of HC-056456 to inhibit evoked Ca2+ entry was examined. In Figs. 3A–C, fura-2 reported the spatially-averaged [Ca2+]i of sperm during challenge with a paired-stimulus protocol. Medium K8.6 evoked averaged rates of rise of 8.7 and 6.6 nM Δ[Ca2+]i s−1 during the first and second stimuli when no inhibitor was present. When 3 µM HC-056456 was applied after the first stimulus, the averaged rate decreased from ∼7.5 to ∼1.6 nM Δ[Ca2+]i s−1. When 10 µM HC-056456 was applied after the first stimulus, the averaged rate decreased more strongly, from ∼7.0 to ∼0.7 nM Δ[Ca2+]i s−1. Hence HC-056456 is an effective inhibitor of the CatSper Ca2+ channel activity that is evoked by alkaline depolarization. Fig. 3D shows that at 10 µM the HC-056456 also strongly decreased the rise in [Na+]i that was evoked by removal of external Ca2+. The rates of rise before and during exposure to HC-056456 were ∼0.03 and ∼0.01 ΔRSBFI min−1. Reference: PLoS One. 2009; 4(8): e6844. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2729922/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 150.0 | 489.7 |
The following data is based on the product molecular weight 306.31 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | N/A |
| In vitro protocol: | N/A |
| In vivo protocol: | 1. Carlson AE, Burnett LA, del Camino D, Quill TA, Hille B, Chong JA, Moran MM, Babcock DF. Pharmacological targeting of native CatSper channels reveals a required role in maintenance of sperm hyperactivation. PLoS One. 2009 Aug 31;4(8):e6844. doi: 10.1371/journal.pone.0006844. PMID: 19718436; PMCID: PMC2729922. |
1: Carlson AE, Burnett LA, del Camino D, Quill TA, Hille B, Chong JA, Moran MM, Babcock DF. Pharmacological targeting of native CatSper channels reveals a required role in maintenance of sperm hyperactivation. PLoS One. 2009 Aug 31;4(8):e6844. doi: 10.1371/journal.pone.0006844. PubMed PMID: 19718436; PubMed Central PMCID: PMC2729922.
