2,2,2-trideuterio-1-[4-[4-[[(2R,4S)-2-(2,4-dichlorophenyl)-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]ethanone Property

storage temp. 

Store at -20°C

solubility 

Chloroform: slightly soluble; Methanol: slightly soluble

form 

A solid

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H301Toxic if swalloed

H360May damage fertility or the unborn child

H373May cause damage to organs through prolonged or repeated exposure

H400Very toxic to aquatic life

H410Very toxic to aquatic life with long lasting effects

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P273Avoid release to the environment.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

P308+P313IF exposed or concerned: Get medical advice/attention.

P314Get medical advice/attention if you feel unwell.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P391Collect spillage. Hazardous to the aquatic environment

P405Store locked up.

P501Dispose of contents/container to..…

2,2,2-trideuterio-1-[4-[4-[[(2R,4S)-2-(2,4-dichlorophenyl)-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]ethanone Chemical Properties,Usage,Production

Description

Ketoconazole-d₃ is intended for use as an internal standard for the quantification of ketoconazole by GC- or LC-MS. Ketoconazole is a broad-spectrum triazole antifungal agent that has activity against C. albicans, C. krusei, C. tropicalis, C. glabrata, C. parapsilosis, C. neoformans, and A. fumigatus strains (IC₅₀s = 0.031-8 μg/ml).¹ It inhibits the fungal cytochrome P450 (CYP) isoform CYP51, also known as lanosterol 14α-demethylase, which arrests ergosterol biosynthesis at the fungal membrane. Ketoconazole also inhibits human CYP3A4 (IC₅₀ = 0.54 μM). Formulations containing ketoconazole have been used in the treatment of fungal infections.

Uses

Ketoconazole-d3 is the labeled analogue of Ketoconazole (K186000), which inhibits cytochrome P-450 dependent steps in the biosynthesis of steroid hormones in vivo. Antimetastatic and antineoplastic activity. Orally active 5-lipoxygenase and thromboxane synthase inhibitor.

References

1. Dilmaghanian, S., Gerber, J.G., Filler, D.G., et al. Enantioselectivity of inhibition of cytochrome P450 3A4 (CYP3A4) by ketoconazole: Testosterone and methadone as substrates Chirality 16(2),79-85(2004).