Danazol

Danazol Structure
Danazol structure
Common Name Danazol
CAS Number 17230-88-5 Molecular Weight 337.455
Density 1.2±0.1 g/cm3 Boiling Point 478.2±45.0 °C at 760 mmHg
Molecular Formula C22H27NO2 Melting Point 224.4-226.8ºC
MSDS Chinese USA Flash Point 243.0±28.7 °C
Symbol GHS07 GHS08
GHS07, GHS08
Signal Word Warning

Fasted-state simulated intestinal fluid "FaSSIF-C", a cholesterol containing intestinal model medium for in vitro drug delivery development.

J. Pharm. Sci. 104 , 2213-24, (2015)

A set of biorelevant media "fasted-state simulated intestinal fluid with cholesterol (FaSSIF-C)" for the in vitro study of intestinal drug dissolution in the duodenum was developed. These contain cholesterol at the same levels as in human bile: the cholestero...

Non-linear increases in danazol exposure with dose in older vs. younger beagle dogs: the potential role of differences in bile salt concentration, thermodynamic activity, and formulation digestion.

Pharm. Res. 31(6) , 1536-52, (2014)

To explore the possibility that age-related changes in physiology may result in differences in drug bioavailability after oral administration of lipid based formulations of danazol.Danazol absorption from lipid formulations with increasing drug load was exami...

An in vitro digestion test that reflects rat intestinal conditions to probe the importance of formulation digestion vs first pass metabolism in Danazol bioavailability from lipid based formulations.

Mol. Pharm. 11(11) , 4069-83, (2014)

The impact of gastrointestinal (GI) processing and first pass metabolism on danazol oral bioavailability (BA) was evaluated after administration of self-emulsifying drug delivery systems (SEDDS) in the rat. Danazol absolute BA was determined following oral an...

Practical method for preparing nanosuspension formulations for toxicology studies in the discovery stage: formulation optimization and in vitro/in vivo evaluation of nanosized poorly water-soluble compounds.

Chem. Pharm. Bull. 62(11) , 1073-82, (2014)

The present study aimed to develop a practical method for preparing nanosuspension formulations of poorly water-soluble compounds for enhancing oral absorption in toxicology studies in the discovery stage. To obtain a suitable nanosuspension formulation for t...

Hematopoietic stem/progenitor cells express several functional sex hormone receptors-novel evidence for a potential developmental link between hematopoiesis and primordial germ cells.

Stem Cells Dev. 24(8) , 927-37, (2015)

Evidence has accumulated that hematopoietic stem progenitor cells (HSPCs) share several markers with the germline, a connection supported by reports that prolactin, androgens, and estrogens stimulate hematopoiesis. To address this issue more directly, we test...

Food Effect in Humans: Predicting the Risk Through In Vitro Dissolution and In Vivo Pharmacokinetic Models.

AAPS J. 17 , 988-98, (2015)

In vitro and in vivo experimental models are frequently used to assess a new chemical entity's (NCE) biopharmaceutical performance risk for food effect (FE) in humans. Their ability to predict human FE hinges on replicating key features of clinical FE studies...

Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.

Drug Metab. Dispos. 40(5) , 943-51, (2012)

CYP2J2, an arachidonic acid epoxygenase, is recognized for its role in the first-pass metabolism of astemizole and ebastine. To fully assess the role of CYP2J2 in drug metabolism, a selective substrate and potent specific chemical inhibitor are essential. In ...

Danazol Inhibits Cytochrome P450 2J2 Activity in a Substrate-independent Manner.

Drug Metab. Dispos. 43 , 1250-3, (2015)

Cytochrome P450 2J2 (CYP2J2) is an enzyme responsible for the metabolism of endogenous substrates including arachidonic acid, as well as therapeutic drugs such as albendazole, astemizole, ebastine, and terfenadine. Selective inhibitors of CYP2J2 are essential...

In Vitro Hepatic Oxidative Biotransformation of Trimethoprim.

Drug Metab. Dispos. 43 , 1372-80, (2015)

Trimethoprim (TMP) has been widely used since the 1960s, both alone and in combination with sulfamethoxazole. Unfortunately, information regarding the role that cytochrome P450 enzymes (P450s) play in the formation of TMP primary metabolites is scarce. Hence,...

An integrated ceramic, micro-fluidic device for the LC/MS/MS analysis of pharmaceuticals in plasma.

Analyst 140 , 5546-56, (2015)

An integrated capillary scale (300 μm id) ceramic microfluidic LC system combined with MS/MS has been successfully employed for the quantitative analysis of pharmaceutical compounds in human plasma. The capillary ceramic microfluidic LC/MS/MS system showed an...