An inhibitor of the 3β-HSDs: 3β-HSD1 and 3β-HSD2 (Kis = 0.10 and 1.60 μM

Trilostane – 5 mg

Brand:
Cayman
CAS:
13647-35-3
Storage:
-20
UN-No:
Non-Hazardous - /

3β-hydroxysteroid dehydrogenase (3β-HSD) type 1 and type 2 isoforms are key enzymes for the biosynthesis of all active steroid hormones. 3β-HSD1 (type I) is expressed in placenta and peripheral tissues including breast tumors, whereas 3β-HSD2 (type 2) is expressed in the adrenal gland, ovary, and testis. Trilostane is an inhibitor of the 3β-HSDs: 3β-HSD1 and 3β-HSD2 with Ki values of 0.10 and 1.60 μM, respectively.{22379} Trilsotane has been approved for use in the treatment of Cushing’s syndrome in dogs to reduce cortisol, aldosterone, and corticosterone levels.{22378} Because human 3β-HSD (type 1) is a critical enzyme in the conversion of DHEA to estradiol in breast tumors, trilostane is also of interest for the treatment of breast cancer in postmenopausal women.{22377}  

 

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Description

An inhibitor of the 3β-HSDs: 3β-HSD1 and 3β-HSD2 (Kis = 0.10 and 1.60 μM, respectively); approved for use in reducing cortisol, aldosterone, and corticosterone levels in dogs diagnosed with Cushing’s syndrome; may potentially benefit the treatment of breast cancer in postmenopausal women

Formal name: 4α,5α-epoxy-3,17β-dihydroxy-androst-2-ene-2-carbonitrile

Synonyms:  Desopan|Modrefen|Vetoryl|WIN 24,540

Molecular weight: 329.4

CAS: 13647-35-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Lipids|Sterol Lipids||Product Type|Biochemicals|Small Molecule Inhibitors|Sterol Biosynthesis||Research Area|Cancer||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Glucocorticoids & Mineralocorticoids||Research Area|Lipid Biochemistry|Sterol Lipids

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