1. Anti-infection
    Metabolic Enzyme/Protease
  2. Fungal
    Cytochrome P450
  3. Ketoconazole

Ketoconazole (Synonyms: Ketoconazol; R 41400)

Cat. No.: HY-B0105 Purity: 99.67%
Handling Instructions

Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.

For research use only. We do not sell to patients.

Ketoconazole Chemical Structure

Ketoconazole Chemical Structure

CAS No. : 65277-42-1

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5 g USD 406 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.

IC50 & Target

CYP3A4, CYP24A1.

In Vitro

Ketoconazole (R-41400), 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 (R-41400) also is a cytochrome P450 inhibitor[2]. Ketoconazole (R-41400), 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]. CYP24A1 inhibitor enhances antiproliferative effects, increases systemic calcitriol exposure, and promotes the activation of caspase-independent apoptosis pathway[4].

Clinical Trial
Molecular Weight

531.43

Formula

C₂₆H₂₈Cl₂N₄O₄

CAS No.

65277-42-1

SMILES

CC(N1CCN(C2=CC=C(OC[[email protected]@H]3O[[email protected]@](CN4C=CN=C4)(C5=CC=C(Cl)C=C5Cl)OC3)C=C2)CC1)=O.[relative stereochemistry]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 53 mg/mL (99.73 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8817 mL 9.4086 mL 18.8172 mL
5 mM 0.3763 mL 1.8817 mL 3.7634 mL
10 mM 0.1882 mL 0.9409 mL 1.8817 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

KetoconazoleKetoconazolR 41400R41400R-41400FungalCytochrome P450CYPsInhibitorinhibitorinhibit

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