Ketoconazole CAS#65277-42-1
Broad-Spectrum Antifungal Activity – Ketoconazole is an imidazole antifungal effective against a wide range of fungal infections, including superficial and deep mycoses.
Selective Inhibition of Ergosterol Biosynthesis – It blocks ergosterol synthesis by interfering with fungal cytochrome P-450, disrupting cell membranes and preventing fungal growth.
Prevention of Fungal Growth and Spore Transformation – Ketoconazole inhibits fungal growth and prevents spores from forming mycelium, reducing reinfection risk.
Antibacterial and Clinical Versatility – It acts against Candida, Coccidioides, Histoplasma, Sporothrix, and Trichophyton, and is used to treat tinea pedis, tinea corporis, tinea cruris, thrush, and skin candidiasis.
Products Description of Ketoconazole CAS#65277-42-1
Ketoconazole is a broad-spectrum antifungal drug of the imidazole class, commercially known as Jindaconin, Mikangling, and Kening. It works by selectively inhibiting fungal cytochrome P-450, thereby blocking ergosterol biosynthesis in fungal cell membranes. This action disrupts membrane integrity and is effective against both superficial and deep fungal infections. Ketoconazole not only suppresses fungal growth but also prevents spores from transforming into mycelium, reducing the risk of reinfection. At low concentrations, it inhibits bacterial growth, while at higher concentrations it exhibits bactericidal activity. It is effective against pathogens such as Candida, chromophores, Coccidioides, Histoplasma, Sporothrix, and Trichophyton, and is clinically used to treat conditions including tinea manuum, tinea pedis, skin tinea, tinea corporis, tinea cruris, thrush, tinea versicolor, and skin candidiasis.
Parameters
| Melting point | 148-152 °C |
| Boiling point | 753.4±60.0 °C(Predicted) |
| density | 1.4046 (rough estimate) |
| refractive index | -10.5 ° (C=0.4, CHCl3) |
| Fp | 9℃ |
| storage temp. | 2-8°C |
| solubility | methanol: soluble50mg/mL |
| pka | pKa 3.25/6.22(H2O,t =25,I=0.025) (Uncertain) |
| form | Off-white solid |
| color | white to light yellow |
| optical activity | [α]20/D -1 to 1°, c = 4 in methanol |
| Water Solubility | Soluble in DMSO, ethanol, chloroform, water, and methanol. |
| Merck | 145302 |
| BCS Class | 2 |
| Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| InChIKey | XMAYWYJOQHXEEK-OZXSUGGESA-N |
| LogP | 4.35 |
| CAS DataBase Reference | 65277-42-1(CAS DataBase Reference) |
Safety Information
| Hazard Codes | T,N,F |
| Risk Statements | 25-36/37/38-23/24/25-50/53-48/22-60-39/23/24/25-11 |
| Safety Statements | 36-45-36/37/39-26-61-60-53-36/37-16-7 |
| RIDADR | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| RTECS | TK7912300 |
| HazardClass | 6.1(b) |
| PackingGroup | III |
| HS Code | 29349990 |
| Hazardous Substances Data | 65277-42-1(Hazardous Substances Data) |
| Toxicity | LD50 in mice, rats, guinea pigs, dogs (mg/kg): 44, 86, 28, 49 i.v.; 702, 227, 202, 780 orally (Heel) |
Product Application of Ketoconazole CAS#65277-42-1
Ketoconazole is an imidazole-class antifungal drug with broad-spectrum activity. It is commonly used to treat conditions such as athlete’s foot, dandruff, candidiasis, chronic mucocutaneous candidiasis, oral thrush, candiduria, blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis. As a CYP3A4 inhibitor, it is also employed in pharmacological studies to evaluate p-glycoprotein/CYP3A-limited bioavailability in animal models, investigate interleukin-1-mediated antitumor effects, and examine in vivo drug interactions.



