Physicochemical Properties
| CAS # | 2946669-78-7 |
| Appearance | Typically exists as solid at room temperature |
| HS Tariff Code | 2934.99.9001 |
| 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) |
Biological Activity
| ln Vitro | For mammalian cells, S-F24 (10-30 μM, 48 h) exhibits lower toxicity [1]. The MIC80 value against C. albicans SC5314 is increased eight-fold by S-F24 (0.002 μg/mL, 20 passes) [1]. In C. albicans SC5314, ergosterol production is 92.03% inhibited by S-F24 (0.004 μg/mL, 16 h)[1]. |
| ln Vivo | For the treatment of C in female IRC mice, S-F24 (1,5 mg/kg, ip, once day for five days) is frequently employed. albicans SC5314, A. fungus resistant to C, fumigatus CGMCC3.7795, and others. 24D Candida albicans Invasive infection[1]. When used in combination with C, S-F24 (0.5, 1 mg/kg, ip, once daily for 5 days) effectively inhibits skin infections. female IRC mice harboring albicans SC5314 [1]. |
| Cell Assay |
Cell Cytotoxicity Assay[1] Cell Types: HUVEC, MCF-10A, 16HBE, LO2 Tested Concentrations: 0.4 μM, 10-30 μM Incubation Duration: 48 h Experimental Results: Displayed weak cytotoxicity with IC50 values ranging from 13.97 to 29.22 μM. Inhibited CYP3A4 with an IC50 value of 0.4 μM. |
| Animal Protocol |
Animal/Disease Models: ICR mouse models infected systemically with C. albicans SC5314, or A. fumigatus CGMCC3.7795, or multi-resistant C. albicans 24D[1] Doses: 1, 5 mg/kg/day, continue for 5 days Route of Administration: intraperitoneal (ip)injection Experimental Results: Increased the median survival time (MST) to 6 days at 1.0 mg/kg/day in C. albicans SC5314 challenge. Increased the MST in a dose-dependent manner Dramatically in fumigatus CGMCC3.7795 challenge. Increased the MST to 12 days at 1.0 mg/kg/day in multi-resistant C. albicans 24D challenge. Animal/Disease Models: C. albicans[1]. Doses: 0.5, 1 mg/kg/day, continue for 5 days Route of Administration: intraperitoneal (ip)injection Experimental Results: diminished the fungal burden Dramatically and demonstrated better therapeutic effects than the Luli (HY-14283) (1 mg/kg) group. Inhibited fungi almost completely in the group at 1.0 mg/kg. |
| References | [1]. Zhu P, et al. Novel Triazoles with Potent and Broad-Spectrum Antifungal Activity In Vitro and In Vivo. J Med Chem. 2023 Jun 8;66(11):7497-7515. |
Solubility Data
| Solubility (In Vitro) | May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples |
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *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. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |