CB-03-01

CB-03-01

CB-03-01 (commercially recognized in clinical literature as Clascoterone or Cortexolone 17α-propionate) is a synthetic pregnane steroid derivative that functions as a selective steroidal androgen receptor (AR) antagonist. Structurally optimized via the esterification of 11-deoxycortisol at the C17α position, this investigational compound serves as a critical reference ligand in competitive binding assays and structural pharmacology research. Because it possesses a localized mechanism of action that undergoes rapid biological hydrolysis upon cellular entry into its parent form (cortexolone), CB-03-01 is actively studied to map the precise boundaries of targeted, peripherally selective anti-androgenic activity without causing broad systemic hormone suppression.

Technical Specifications

Research Applications & Mechanism of Interest

In molecular medicine and receptor pharmacology frameworks, CB-03-01 provides a high-affinity competitive template for evaluating the mechanics of the human androgen receptor’s ligand-binding domain. Data published in the Journal of Drugs in Dermatology highlights its sub-micromolar binding capacity (IC₅₀ value of approximately 0.4 to 1 µM), effectively competing against native dihydrotestosterone (DHT) and testosterone to block downstream AR nuclear translocation.

Primary fields of investigative laboratory research include:

• Androgen Receptor Binding Kinematics: Executing competitive displacement assays in cell-free environments to determine the exact structural contributions of the propionate group to steric fitting within the hydrophobic pocket of receptor proteins.

• Transcriptional Modulation Mapping: Observing in vitro systems to track how localized antagonist introduction alters the expression of androgen-responsive target genes and transcription factors without modifying systemic endocrine baselines.

• Lipid and Cytokine Signaling Assays: Utilizing human primary sebocyte cultures to monitor the inhibition of androgen-stimulated lipid synthesis and pro-inflammatory cytokine cascades under controlled conditions.

• Co-Solute and Carrier Behavior Analysis: Conducted to observe the thermodynamic properties, micellar interaction boundaries, and stable concentration parameters of the steroid matrix when evaluated across diverse vehicle environments.

Storage & Handling Guidelines

To maintain absolute chemical uniformity and guard against premature hydrolysis or structural shifting during analytical assays:

• Temperature Maintenance: Store the pristine material at room temperature (or continuously cold at 2–8°C for extended structural stability, depending on specific laboratory reconstitution timelines).

• Environmental Controls: Keep containers tightly sealed directly after use to eliminate any moisture introduction or ambient air exchange that could compromise the ester bond.

• Photolytic Isolation: Shield completely from localized heat arrays and direct sunlight by housing inside opaque or high-grade amber laboratory containment vessels.

• Aseptic Manipulation: Always employ strict laboratory personal protective equipment (PPE) and use sterile instruments during standard extraction and deployment protocols.

Research Use Only Disclaimer: This product is distributed, manufactured, and sold strictly as a Research Use Only (RUO) laboratory reference chemical. It is not an FDA-approved drug, medication, active pharmaceutical ingredient, or dietary supplement, and is strictly prohibited for human or animal consumption. Kimera Chems provides these reference standards exclusively to accredited institutional laboratories and certified scientific investigators for in vitro analytical research.

Frequently Asked Research Questions

How does CB-03-01 block androgen signaling at the cellular level?

In preclinical assays, CB-03-01 competes directly with endogenous androgens like DHT for the ligand-binding core of the androgen receptor. By locking the receptor in an inactive state, it actively interrupts the nuclear translocation step required to prompt the transcription of androgen-dependent genes.

What is the significance of the 17α-propionate ester modification?

The propionate ester group fundamentally alters both the lipophilicity and the metabolism profile of the compound. While it enhances membrane permeability during cell-free evaluations, cellular esterases rapidly cleave this bond to yield cortexolone, an inactive metabolite that provides a clean model for studying peripherally selective signaling.

Scientific References

1. Celasco, G., Moro, L., Bozzella, R., Ferraboschi, P., Bartorelli, L., Quattrocchi, C., & Nicoletti, F. (2004). “Pharmacological profile of 17α-propionate of cortexolone (CB-03-01), a new topical antiandrogen.” Arzneimittelforschung, 54(12), 881–886. DOI: 10.1055/s-0031-1297043.

2. Rosette, C., Agan, F. J., Mazzetti, A., Moro, L., & Kasmsieh, W. (2019). “Cortexolone 17α-Propionate (Clascoterone) Is a Novel Androgen Receptor Antagonist that Inhibits Production of Lipids and Inflammatory Cytokines in Sebocytes.” Journal of Drugs in Dermatology, 18(5), 412–418. PMID: 31141847.