Exemestane 25 mg

Exemestane is a synthetic small molecule belonging to the class of steroidal enzyme inactivators, chemically an androstadienedione with an exocyclic methylidene group. In scientific research, it is studied as a model compound for mechanism-related enzyme inhibition and as a reference standard in analytical work. This compound is offered as 25 mg tablets, exclusively for laboratory and research purposes.

What is Exemestane?

Exemestane (6-methylideneandrosta-1,4-diene-3,17-dione) is composed of the classic quadruple steroid backbone with two ketone functions, a conjugated diene in the A-ring, and an extra methylidene group at position 6. This exocyclic double bond, directly adjacent to a carbonyl group, makes the molecule a weak Michael acceptor: an electron-rich center in the vicinity can bind to it covalently. Because the rest of the structure closely resembles the natural substrate androstenedione, the compound combines substrate recognition with chemical reactivity; it is precisely this property that makes it a favorite model in enzyme kinetic research.

In research models, Exemestane is accepted as a substrate by the enzyme aromatase (CYP19A1), after which it forms a covalent bond in the active cavity and irreversibly disables the enzyme. This behavior, referred to in the literature as mechanism-related or suicide inactivation, proceeds fundamentally differently from reversible, competitive inhibition by triazole compounds. Consequently, the substance provides a clear distinguishing reference point in microsome and cell models. Within scientific research, Exemestane is therefore used as a model compound and reference substance.

Aree di ricerca

In a laboratory context, Exemestane occurs in the following research areas, among others:

• Enzyme kinetic research into time-dependent, irreversible inactivation of CYP19A1 in microsome models.
• Substrate competition study in which the compound is plotted against the natural substrate androstenedion.
• Research into steroid conversion in cell culture systems, monitored via the conversion products in the culture medium.
• Comparative mechanism study between steroidal inactivators and reversible non-steroidal inhibitors.
• Analytical method development and validation (HPLC, LC-MS, APCI ionization) using Exemestane as the reference standard for neutral steroids.
• Stability and solubility studies of nonpolar steroid structures under controlled conditions.

Ciascuna di queste applicazioni prevede ricerche controllate in laboratorio o su modelli preclinici.

Exemestane in our research assortment

Exemestane falls under the category of oral investigational compounds in solid tablet form within our range. Researchers working with this category regularly place the compound alongside other small molecules that are studied via their own biochemical targets. While Exemestane focuses on irreversible, substrate-bound enzyme inactivation, other components within the same product line have been chosen specifically to cover reversible enzyme inhibition or receptor-bound targets. These compounds share the solid tablet form and the standardized amount of active substance per unit, but differ fundamentally in molecular class and the mechanism under investigation.

Specifiche

Forma, manipolazione e stoccaggio

Exemestane is supplied as solid tablets with a standardized amount of 25 mg per tablet, packed in units of 100. The solid form can be weighed directly in a laboratory setup; for chromatographic work, the material is incorporated into a suitable organic medium, because the neutral steroid structure contains hardly any ionizable groups and is therefore poorly miscible with purely aqueous media.

Store the tablets dry at room temperature, protected from direct light and moisture, in the original packaging. The conjugated diene-ketone structure is sensitive to light and oxidation, so a dark, dry storage location best preserves the structure. Handle the compound with standard laboratory precautions: work in a clean environment, use appropriate personal protective equipment, and prevent cross-contamination with other research materials. Keep the packaging out of reach of unauthorized persons.

Composizione e risultati di laboratorio

For this compound, the content is expressed as the amount of active substance per tablet (25 mg per tablet) rather than as a purity percentage, as is customary for tablet and capsule formulations. The relevant specification is therefore the uniform distribution of the active substance across the units.

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Domande frequenti

To which class of substances does Exemestane belong?
Exemestane is a steroidal compound derived from the androstan skeleton and is classified as a mechanism-linked aromatase inactivator of type I. It is not a peptide and therefore contains no amino acid sequence.

What makes the inactivation irreversible?
The methylidene group at position 6 is adjacent to a carbonyl group and therefore acts as a weak Michael acceptor. After the enzyme has accepted the compound as a substrate, a covalent bond forms in the active cavity, causing the enzyme molecule to remain permanently inactive in research models instead of becoming available again after dilution.

In quale forma viene fornito il composto?
As solid tablets with 25 mg of active substance per tablet, packed in units of 100.

Come conservo le compresse?
Conservare asciutto, a temperatura ambiente e al riparo dalla luce e dall'umidità, preferibilmente nella confezione originale.