(+) -Ketoconazole

• Description :

  (+) -Ketoconazole ((+) -R 41400) is an imidazole anti-fungal agent, a CYP3A4 inhibitor. Target: CYP3A4 (+) -Ketoconazole, an imidazole anti-fungal agent, has often produced features of androgen deficiency including decreased libido, gynecomastia, impotence, oligospermia, and decreased testosterone levels, in men being treated for chronic mycotic infections [1]. (+) -Ketoconazole also is a cytochrome P450 inhibitor [2]. (+) -Ketoconazole (KTZ), on the antischistosomal potential of these quinolines against Schistosoma mansoni infection by evaluating parasitological, histopathological, and biochemical parameters. Mice were classified into 7 groups: uninfected untreated (I), infected untreated (II), infected treated orally with PZQ (1,000 mg/kg) (III), QN (400 mg/kg) (IV), KTZ (10 mg/kg) +QN as group IV (V), HF (400 mg/kg) (VI), and KTZ (as group V) +HF (as group VI) (VII) . KTZ plus QN or HF produced more inhibition (P<0.05) in hepatic CYP450 (85.7% and 83.8%) and CYT b5 (75.5% and 73.5%) activities, respectively, than in groups treated with QN or HF alone. This was accompanied with more reduction in female (89.0% and 79.3%), total worms (81.4% and 70.3%), and eggs burden (hepatic; 83.8%, 66.0% and intestinal; 68%, 64.5%), respectively, and encountering the granulomatous reaction to parasite eggs trapped in the liver [3]. Clinical indications: Candida infection; Dermatophytosis; Folliculitis FDA Approved Date: Toxicity: teratogenesis; liver injuries; adrenal gland problems

• Product Name Alternative :

  (+) -Ketoconazol; (+) -R 41400

• UNSPSC :

  12352005

• Hazard Statement :

  H315, H319, H320

• Target :

  Cytochrome P450; Fungal

• Type :

  Reference compound

• Related Pathways :

  Anti-infection; Metabolic Enzyme/Protease

• Applications :

  COVID-19-immunoregulation

• Field of Research :

  Infection

• Assay Protocol :

  https://www.medchemexpress.com/__addition__-ketoconazole.html

• Purity :

  99.79

• Solubility :

  DMSO : 33.33 mg/mL (ultrasonic)

• Smiles :

  ClC(C=C1)=CC(Cl)=C1[C@@]2(CN3C=CN=C3)OC[C@H](COC4=CC=C(N5CCN(C(C)=O)CC5)C=C4)O2

• Molecular Formula :

  C26H28Cl2N4O4

• Molecular Weight :

  531.43

• Precautions :

  H315, H319, H320

• References & Citations :

  [1]Eil C. Ketoconazole binds to the human androgen receptor. Horm Metab Res. 1992 Aug;24 (8) :367-70.|[2]Seif El-Din SH, et al. Effect of ketoconazole, a cytochrome P450 inhibitor, on the efficacy of quinine and halofantrine against Schistosoma mansoni in mice. Korean J Parasitol. 2013 Apr;51 (2) :165-75.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Launched

• Isoform :

  CYP3

• CAS Number :

  [142128-59-4]