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Postion:Product Catalog >API>Synthetic Anti-infective Drugs>Antifungal Drugs>Ketoconazole
Ketoconazole
  • Ketoconazole

Ketoconazole NEW

Price $33 $46 $72
Package 50mg 100mg 500mg
Min. Order:
Supply Ability: 10g
Update Time: 2025-05-02

Product Details

Product Name: Ketoconazole CAS No.: 65277-42-1
Purity: 99.61% Supply Ability: 10g
Release date: 2025/05/02

Product Introduction

Bioactivity

NameKetoconazole
DescriptionKetoconazole (R-41400), a CYP3A4 inhibitor, is an imidazole anti-fungal agent.
Cell ResearchHT29-S-B6 cells (5×105) are plated in 35-mm Petri dishes. The next day, the medium is changed and effectors are added in a small volume (10-20 μL). The incubation medium is renewed every day during the experiments. The same triplicate dishes are used for cell counts, [3H]thymidine incorporation, and flow cytometry. [3H]Thymidine (0.5 μCi) is allowed to incorporate for 24 hours; at the end of incubation, cells are rinsed with 1 mL of medium, detached with 1 mL of trypsin-EDTA, and diluted (1:3) with the culture medium. An aliquot (0.5-1 mL) is used for cell count with a Coulter Counter.(Only for Reference)
Kinase AssayWhole Cell [3H]R1881 Binding Assay: Fibroblasts are grown to confluence in five or six 150 cm2 tissue culture flasks for routine assay. This usually requires 4-6 weeks from the time of the initial seeding of the cell line. All studies are performed between passages 3-20. Two days before assay, the medium is changed to one lacking fetal calf serum. This is repeated again 24 hours before assay. Competition assays are performed with 0.5-1.0 nM [3H]R1881 and increasing amounts of the nonradioactive compounds. Binding to low affinity sites is determined in the presence of 5 × 10-7 M R1881 and is subtracted from whole cell binding of [3H]R 1881 obtained in the absence of any inhibitor to assess binding to 5 high affinity site
In vitroIntraperitoneal administration of Ketoconazole (25 mg/kg) in rats significantly reduced plasma corticosterone levels and decreased self-administration of low doses of cocaine. Rats treated with Ketoconazole exhibited enhanced bioavailability of digoxin, increasing from 0.68 to 0.84, with the mean absorption time decreasing from 1.1 h to 0.3 h. Moreover, the oral area under the curve (AUC) for digoxin increased from 63 mg·h/L to 411 mg·h/L, while the intravenous AUC also rose from 93 mg·h/L to 486 mg·h/L.
In vivoIn HT29-S-B6 colorectal cancer cells, Ketoconazole decreased cell proliferation and [3H]thymidine uptake in a dose-dependent manner, with an IC50 of 2.5 mM. Ketoconazole also inhibited [3H]thymidine uptake in both Evsa-T and MDA-MB-231 cell lines, with respective IC50 values of 2 μM and 13 μM. Within 24 hours, Ketoconazole induced a dose-dependent reduction in the S-phase cell population (from 17% to 3%) and a corresponding increase in the Go-G1 phase cell percentage (from 64% to 80%) in HT29-S-B6 cells. By competitively binding with [3H]Dexamethasone, Ketoconazole inhibited fibroblast glucocorticoid receptors, with an IC50 of 0.3 mM. Several Aspergillus species were sensitive to Ketoconazole, with a minimum inhibitory concentration of 0.03 μg/mL.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information10% DMSO+40% PEG300+5% Tween 80+45% Saline : 0.53 mg/mL (1 mM), In vivo: Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
DMSO : 5.31 mg/mL (10 mM), Sonication is recommended.
KeywordsTestosterone 6 beta-hydroxylase | Steroid 21-hydroxylase | Ras | R41400 | R 41400 | NADPHoxidase | Ketoconazole | Ketoconazol | Inhibitor | inhibit | Fungal | Cytochrome P450 | CYPs | CYP3A4 | CYP24A1 | Cyclosporine oxidase | 17-hydroxylase | 12-hydroxylase
Inhibitors RelatedDehydroacetic acid sodium | Chlorobutanol hemihydrate | 2-Butyl-1,2-benzisothiazolin-3-one | Tebuconazole | Potassium gluconate | Chitosan (MW 150000) | Methyl 2-amino-5-bromobenzoate | Paclobutrazol | Lauryl betaine | Geraniol | Naringin | Naringenin
Related Compound LibrariesFailed Clinical Trials Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | FDA-Approved Kinase Inhibitor Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | GPCR Compound Library | Anti-Cancer Drug Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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  • Since: 2011-01-07
  • Address: 36 Washington Street, Wellesley Hill, USA
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