Ketoconazole (R 41400) - Moligand™, 2mM in DMSO , Inhibitor of CYP3A4;Channel blocker of K v1.8, CAS No.65277-42-1, Inhibitor of CYP3A4;Channel blocker of K v1.8

CAS: 65277-42-1 Cat. No.: K408590 Peso molecular: 531.43 Número EC: 265-667-4

GRADE & PURITY Moligand™, 2mM in DMSO

Synonyms

1-(4-(4-(((2R,4S)-2-((1H-imidazol-1-yl)methyl)-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl)methoxy)phenyl)piperazin-1-yl)ethanone

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Ketoconazole (R 41400) inhibitscyclosporine oxidaseandtestosterone 6 beta-hydroxylasewithIC50of 0.19 mM and 0.22 mM, respectively. Ketoconazole is anandrogenbiosynthesis inhibitor.
In vitro

Ketoconazole interacts with androgen receptors in a competitive fashion in intact human foreskin fibroblasts. Ketoconazole competes for [³H]dexamethasone binding to fibroblast glucocorticoid receptors with IC50 of 0.3 mM. Ketoconazole reduces cell proliferation and [³H]thymidine incorporation with IC50 of 2.5 mM in the serum independent HT29-S-B6 colon cell clone. Ketoconazole inhibits the incorporation of [³H]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.
Cell Data

cell lines：

Concentrations：25 μM

Incubation Time：72 hours

Powder Purity:≥99%

Specifications

Sinónimos

1-(4-(4-(((2R, 4S)-2-((1H-imidazol-1-yl)methyl)-2-(2, 4-dichlorophenyl)-1, 3-dioxolan-4-yl)methoxy)phenyl)piperazin-1-yl)ethanone

Especificaciones y pureza

Moligand™, 2mM in DMSO

Mecanismos bioquímicos y fisiológicos

Ketoconazole (R 41400) inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively. Ketoconazole is an androgen biosynthesis inhibitor.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

CHANNEL BLOCKER, INHIBITOR

Mecanismo de acción

Inhibitor of CYP3A4;Channel blocker of K v1.8

Nombres e identificadores

• Isómeros SMILES: CC(=O)N1CCN(CC1)C2=CC=C(C=C2)OC[C@H]3CO[C@](O3)(CN4C=CN=C4)C5=C(C=C(C=C5)Cl)Cl
• WGK Alemania: 3
• RTECS: TK7912300
• Peso molecular: 531.43
• Reaxy-Rn: 634785
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=634785&ln=

Objetivos asociados (humanos)

CYP2D6 Tclin Cytochrome P450 2D6 (0 Activities)

Discover Target: CYP2D6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP24A1 Tchem 1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial (0 Activities)

Discover Target: CYP24A1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP3A4 Tclin Cytochrome P450 3A4 (1 Activities)

Discover Target: CYP3A4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP3A5 Tclin Cytochrome P450 3A5 (0 Activities)

Discover Target: CYP3A5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP19A1 Tclin Aromatase (0 Activities)

Discover Target: CYP19A1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP17A1 Tclin Steroid 17-alpha-hydroxylase/17,20 lyase (0 Activities)

Discover Target: CYP17A1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 56 mg/mL (197.02 mM)
• Punto de fusión (°C): 150 °C

Referencias

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