[CAS NO. 65277-42-1] Ketoconazole (R 41400)

Name: Ketoconazole (R 41400)
Brand: Arctom Scientific
SKU: SLK-S1353

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PRODUCTS SPECIFICATIONS [65277-42-1]

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Catalog

SLK-S1353

Brand

Selleck

CAS

65277-42-1

DESCRIPTION [65277-42-1]

Overview

MDL	MFCD00058579
Molecular Weight	531.43
Molecular Formula	C26H28Cl2N4O4
SMILES	C([C@]1(O[C@@H](COC2=CC=C(C=C2)N3CCN(C(C)=O)CC3)CO1)C4=C(Cl)C=C(Cl)C=C4)N5C=CN=C5

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume 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
50 mM	-	-	-

Description

Ketoconazole (R 41400) inhibits and with of 0.19 mM and 0.22 mM, respectively. Ketoconazole is an biosynthesis inhibitor.

Features

More active than both Econazole and Miconazole against Malassezia species.

Targets

Cyclosporine oxidase ^[1]	Testosterone 6 beta-hydroxylase ^[1]
0.19 mM	0.22 mM

In vitro

Ketoconazole interacts with androgen receptors in a competitive fashion in intact human foreskin fibroblasts. Ketoconazole competes for [H]dexamethasone binding to fibroblast glucocorticoid receptors with IC50 of 0.3 mM. Ketoconazole reduces cell proliferation and [H]thymidine incorporation with IC50 of 2.5 mM in the serum independent HT29-S-B6 colon cell clone. Ketoconazole inhibits the incorporation of [H]thymidine with IC50 of 2 μM and 13 μM in the Evsa-T cell line and MDA-MB-231 cell line, respectively. Ketoconazole induces a decrease of the number of cells in S phase and a corresponding increase of the percentage of cells in Go-G1 in HT29-S-B6 cells. Ketoconazole is susceptable to several Malassezia species with minimum inhibitory concentrations (MICs) of 0.03 µg/mL.

In vivo

Ketoconazole (25 mg/kg, i.p.) significantly decreases plasma corticosterone and reduces low dose cocaine self-administration without affecting food-reinforced responding in rats. Ketoconazole raises the AUC of orally administered digoxin from 63 mg x h/L to 411 mg x h/L in rats. Ketoconazole raises the AUC of intravenously administered digoxin from 93 mg × h/L to 486 mg × h/L in rats. Ketoconazole increases digoxin bioavailability from 0.68 to 0.84 in rats, while mean absorption time is reduced from 1.1 hours to 0.3 hour.

References

[1] Oliver WR Jr, et al. Proc Natl Acad Sci U S A, 2001, 98(9), 5306-5311.
[2] Eil C, et al. Horm Metab Res, 1992, 24(8), 367-370.
[3] Forgue-Lafitte ME, et al. Cancer Res, 1992, 52(24), 6827-6831.
[4] Gupta AK, et al. Br J Dermatol, 2000, 142(4), 758-765.
[5] Goeders NE, et al. Drug Alcohol Depend, 1998, 53(1), 67-77.
[6] Salphati L, et al. Pharmacology, 1998, 56(6), 308-313.

Synonyms

Ethanone, 1-[4-[4-[[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]-, rel-

Piperazine, 1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-, cis-

Piperazine, 1-acetyl-4-[4-[[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-, rel-

rel-1-[4-[4-[[(2R,4S)-2-(2,4-Dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]ethanone

Ketoconazole

R 41400

Nizoral

(±)-Ketoconazole

Fungoral

Nizral

Orifungal M

Ketoderm

Panfungol

Ketoisdin

Fungarest

Brizoral

Onofin K

Ketozoral

Phytorol

Tocon

Nizaral

Micosin