Cat. No.: HY-B0105A

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(+)-Ketoconazole

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

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

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

Purity: 99.79%
CAS No.: 142128-59-4
Formula: C₂₆H₂₈Cl₂N₄O₄
Molecular Weight:531.43

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

(+)-Ketoconazole Chemical Structure

CAS No.: 142128-59-4

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Biological Activity
- Description
- Cellular Effect
- Parmacokinetics
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

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

All Cytochrome P450 Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
ASPC1	IC₅₀	0.117 μM Compound: Keto	Inhibition of CYP3A4 in CRISPR/Cas9-mediated CYP3A5 knock-out and doxycycline-induced CYP3A4 overexpressing human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate pretreated with doxycycline for 24 hrs followed Inhibition of CYP3A4 in CRISPR/Cas9-mediated CYP3A5 knock-out and doxycycline-induced CYP3A4 overexpressing human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate pretreated with doxycycline for 24 hrs followed	[PMID: 31965799]
ASPC1	IC₅₀	0.141 μM Compound: Keto	Inhibition of CYP3A5 in doxycycline-induced CYP3A5 overexpressing wild type human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate pretreated with doxycycline for 24 hrs followed by incubation with compound for Inhibition of CYP3A5 in doxycycline-induced CYP3A5 overexpressing wild type human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate pretreated with doxycycline for 24 hrs followed by incubation with compound for	[PMID: 31965799]
ASPC1	IC₅₀	0.162 μM Compound: Keto	Inhibition of CYP3A5 in CRISPR/Cas9-mediated CYP3A5 knock-out and doxycycline-induced CYP3A5 overexpressing human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate pretreated with doxycycline for 24 hrs followed Inhibition of CYP3A5 in CRISPR/Cas9-mediated CYP3A5 knock-out and doxycycline-induced CYP3A5 overexpressing human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate pretreated with doxycycline for 24 hrs followed	[PMID: 31965799]
ASPC1	IC₅₀	0.439 μM Compound: Keto	Inhibition of CYP3A5 in lentiviral pLVX-TRE3G-ZsGreen1-CYP3A5 transduced wild type human AsPC1 cells overexpressing CYP3A5 assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate after 24 hrs by LC-MS/MS analysis Inhibition of CYP3A5 in lentiviral pLVX-TRE3G-ZsGreen1-CYP3A5 transduced wild type human AsPC1 cells overexpressing CYP3A5 assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate after 24 hrs by LC-MS/MS analysis	[PMID: 31965799]
ASPC1	IC₅₀	0.513 μM Compound: Keto	Inhibition of CYP3A5 in wild type human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate after 24 hrs by LC-MS/MS analysis Inhibition of CYP3A5 in wild type human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate after 24 hrs by LC-MS/MS analysis	[PMID: 31965799]
LNCaP	GI₅₀	25 μM Compound: Ketoconazole	Growth inhibition of androgen-sensitive human LNCAP cells incubated for 48 hrs by sulforhodamine B assay Growth inhibition of androgen-sensitive human LNCAP cells incubated for 48 hrs by sulforhodamine B assay	[PMID: 27423983]
NCI-H295R	IC₅₀	0.34 μM Compound: ketoconazole	Inhibition of testosterone synthesis in human NCI-H295R cells by Enzyme immunoassay Inhibition of testosterone synthesis in human NCI-H295R cells by Enzyme immunoassay	[PMID: 34387987]
NCI-H295R	IC₅₀	0.44 μM Compound: ketoconazole	Inhibition of cortisol synthesis in human NCI-H295R cells by Enzyme immunoassay Inhibition of cortisol synthesis in human NCI-H295R cells by Enzyme immunoassay	[PMID: 34387987]
NCI-H295R	IC₅₀	1.4 μM Compound: ketoconazole	Inhibition of aldosterone synthesis in human NCI-H295R cells by Enzyme immunoassay Inhibition of aldosterone synthesis in human NCI-H295R cells by Enzyme immunoassay	[PMID: 34387987]
NCI-H295R	IC₅₀	2.5 μM Compound: ketoconazole	Inhibition of corticosterone synthesis in human NCI-H295R cells by Enzyme immunoassay Inhibition of corticosterone synthesis in human NCI-H295R cells by Enzyme immunoassay	[PMID: 34387987]
NIH3T3	IC₅₀	396 μg/mL Compound: Ketoconazole	Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 29274492]
PC-3	GI₅₀	11.7 μM Compound: Ketoconazole	Growth inhibition of androgen-insensitive human PC3 cells incubated for 48 hrs by sulforhodamine B assay Growth inhibition of androgen-insensitive human PC3 cells incubated for 48 hrs by sulforhodamine B assay	[PMID: 27423983]

Parmacokinetics

Species	Dose	Route	AUC_0-t	AUC_0-∞	T_1/2	V_dss	CL	MRT	C_max	T_max	CL/F	F
Rat^[1]	10 mg/kg	i.v.	17.29 mg·h/L	17.94 mg·h/L	0.661 h	0.707 L/kg	0.590 L/h/kg	1.25 h	/	/	/	/
Rat^[1]	10 mg/kg	p.o.	5.46 mg·h/L	5.59 mg·h/L	0.580 h	/	/	1.54 h	2.72 mg/L	0.930 h	2.36 L/h/kg	31.1 %
Rat^[1]	20 mg/kg	p.o.	8.74 mg·h/L	9.70 mg·h/L	0.674 h	/	/	1.90 h	4.23 mg/L	1.87 h	3.22 L/h/kg	/
Rat^[1]	40 mg/kg	p.o.	38.9 mg·h/L	56.8 mg·h/L	1.04 h	/	/	2.86 h	15.1 mg/L	1.53 h	0.802 L/h/kg	/
Rat^[1]	50 mg/kg	p.o.	44.7 mg·h/L	71.8 mg·h/L	1.23 h	/	/	3.16 h	18.2 mg/L	1.91 h	0.738 L/h/kg	/
Rat^[1]	80 mg/kg	p.o.	56.3 mg·h/L	112 mg·h/L	2.02 h	/	/	5.22 h	20.7 mg/L	2.05 h	0.771 L/h/kg	/

Chemical Information

CAS No. 142128-59-4
Appearance Solid
Molecular Weight 531.43
Formula C₂₆H₂₈Cl₂N₄O₄
Color White to off-white
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
Synonyms

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

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (62.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Eil C. Ketoconazole binds to the human androgen receptor. Horm Metab Res. 1992 Aug;24(8):367-70. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8817 mL	9.4086 mL	18.8172 mL	47.0429 mL
	5 mM	0.3763 mL	1.8817 mL	3.7634 mL	9.4086 mL
	10 mM	0.1882 mL	0.9409 mL	1.8817 mL	4.7043 mL
	15 mM	0.1254 mL	0.6272 mL	1.2545 mL	3.1362 mL
	20 mM	0.0941 mL	0.4704 mL	0.9409 mL	2.3521 mL
	25 mM	0.0753 mL	0.3763 mL	0.7527 mL	1.8817 mL
	30 mM	0.0627 mL	0.3136 mL	0.6272 mL	1.5681 mL
	40 mM	0.0470 mL	0.2352 mL	0.4704 mL	1.1761 mL
	50 mM	0.0376 mL	0.1882 mL	0.3763 mL	0.9409 mL
	60 mM	0.0314 mL	0.1568 mL	0.3136 mL	0.7840 mL

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(+)-Ketoconazole

Anti-Infection Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Antifungal Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Off-patent Drug Library

Bioactive Compound Library Max

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

All Cytochrome P450 Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

(+)-Ketoconazole

Anti-Infection Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Antifungal Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Off-patent Drug Library

Bioactive Compound Library Max

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

All Cytochrome P450 Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

(+)-Ketoconazole Related Classifications

HY-B0105A Related Classifications