RU-58841 | CAS 154992-24-2 | Androgen Receptor Antagonist (Research Use Only) | Knowlux

Product Description

RU-58841, CAS 154992-24-2, is a non-steroidal small-molecule androgen receptor (AR) antagonist supplied by Knowlux for laboratory research use. The systematic name is 4-[3-(4-hydroxybutyl)-4,4-dimethyl-2,5-dioxoimidazolidin-1-yl]-2-(trifluoromethyl)benzonitrile. The molecular formula is C17H18F3N3O3 and the molecular weight is 369.34 g/mol. Unlike the peptide APIs in this catalogue, RU-58841 is a low-molecular-weight organic compound with no amino acid backbone, no disulfide bonds, and no terminal modifications; its structural class is a hydantoin-substituted benzonitrile, and its solubility and stability profile follow small-molecule rather than peptide conventions. Each lot is released with a lot-specific COA and analytical traceability.

Identity and Formula Verification: The formula C17H18F3N3O3 and molecular weight 369.34 are confirmed across MedChemExpress, Selleck, GLPBIO, ChemicalBook, ChemWhat, and CapotChem. One supplier datasheet (InvivoChem) lists the formula as C17H18F3NO3 with MW 369.3442; this entry omits one nitrogen atom relative to the consensus formula and is treated as a typographical error rather than adopted. The SMILES string CC1(C(=O)N(C(=O)N1CCCCO)C2=CC(=C(C=C2)C#N)C(F)(F)F)C and InChIKey ARBYGDBJECGMGA-UHFFFAOYSA-N are consistent across Selleck and MedChemExpress. The CAS 154992-24-2 is the sole registry applied to this compound in commercial listings; no salt-form ambiguity analogous to the peptide acetate/free-base splits has been identified in the sourced data.

Product Parameters

Product Details

1. Overview

RU-58841 is a non-steroidal anti-androgen developed for topical application in androgen-dependent skin disorders. It binds the androgen receptor (AR) competitively and blocks endogenous androgen (testosterone and dihydrotestosterone, DHT) binding, preventing receptor activation and downstream transcriptional signaling. Unlike systemic anti-androgens, topically applied RU-58841 was reported in preclinical models to produce dose-dependent regression of sebaceous gland area at doses as low as 1 microgram per animal while being devoid of anti-androgenic activity on deep accessory sex organs and producing no effect on testosterone levels up to 100 micrograms per animal. This topical selectivity is the pharmacological rationale for its research use in androgenetic alopecia, acne, and hirsutism models. RU-58841 is not approved as a therapeutic or cosmetic product in any jurisdiction, and the material supplied under this specification is strictly research-grade.

2. Receptor Pharmacology and Binding Affinity

RU-58841 functions as a competitive antagonist at the androgen receptor. Reported binding affinities and antagonist potencies vary across assay formats and receptor sources, and the spread is wider than for most peptide targets in this catalogue. A commonly cited IC50 of approximately 100 nM is reported by BenchChem and Ambeed, with Ambeed additionally listing a binding affinity (ka) of 1.1 nM. BindingDB curated data provide orthogonal values from independent assays: an IC50 of 16 nM for antagonist activity at the human AR expressed in MDA-MB-231 cells (assessed as inhibition of DHT-induced response), alongside a second entry reporting an IC50 of 32 nM in the same cell system, and a displacement assay using [3H]dihydrotestosterone that yielded a Ki in the low-nanomolar range. The 16 nM to 100 nM span reflects differences in cell background, receptor expression level, radioligand concentration, and endpoint (binding displacement versus functional antagonism). For assay design, the low-nanomolar binding affinity establishes RU-58841 as a high-affinity AR ligand, and working concentrations should be established empirically in the specific receptor system rather than extrapolated from a single literature IC50.

3. Research Applications

Published pharmacological characterizations describe the following research applications:

• Androgen receptor binding and functional antagonist assays (DHT displacement, AR-responsive reporter gene assays)

• Androgenetic alopecia and hair follicle biology research models (topical anti-androgen activity)

• Sebaceous gland function and acne research models

• Comparative pharmacology of non-steroidal anti-androgens (RU-58841 versus hydroxyflutamide and bicalutamide)

• Prodrug design and topical delivery studies (RU-58841-myristate as a prodrug that is rapidly metabolized to RU-58841 by human foreskin fibroblasts and keratinocytes)

• Reference standard development for HPLC and LC-MS analytical methods

The prodrug literature describes RU-58841-myristate as almost devoid of AR affinity itself, with conversion to the active RU-58841 occurring in skin cells; this has made the RU-58841 scaffold a model system for topical anti-androgen delivery. These descriptions are derived from published research and are provided for scientific reference only.

Quality Control

Purity specifications for RU-58841 span a wider range than for most peptide APIs in this catalogue, and the grade should be matched to the intended assay. Amadis lists 97% purity for its catalogue item. CapotChem, Biorbyt, and CD BioGlyco specify >=98% by HPLC, with CapotChem additionally listing a water content limit of 0.5% Max. ChemicalBook supplier listings offer 99% purity in kilogram-scale packaging. Santa Cruz Biotechnology and Selleck supply higher-purity grades: an SCBT Certificate of Analysis reports 99.5% by HPLC, and Selleck lists a batch purity of 99.99%. A Baiolaibo batch COA reports 98.16% purity. The principal quality consideration for RU-58841 is the absence of a compendial (USP/Ph.Eur.) monograph: specifications are supplier-defined rather than pharmacopoeial, and lot-specific COA data (HPLC chromatogram, MS, and where available NMR) should be reviewed rather than relying on a catalogue purity figure alone. Researchers preparing solutions for quantitative assays should also request residual solvent and water content data, because the compound is hygroscopic in solution and DMSO solubility is sensitive to moisture ingress.

Solubility and Handling

Solubility: RU-58841 is soluble in DMSO and ethanol and insoluble in water. The DMSO solubility values reported across suppliers are more divergent than for most peptide APIs and require careful interpretation. Selleck's batch-tested experimental data report DMSO 74 mg/mL (200.35 mM) and ethanol 74 mg/mL, with the explicit caveat that moisture-contaminated DMSO reduces solubility and that fresh anhydrous DMSO should be used; the recommended stock concentration is 10 mM. MedChemExpress lists DMSO solubility of >=100 mg/mL (270.75 mM) with saturation unknown. GLPBIO lists DMSO >=36.9 mg/mL and ethanol >=87.6 mg/mL. ApexBio lists DMSO >=36.9 mg/mL and ethanol >=87.6 mg/mL, with water insoluble. Adooq and CD BioGlyco list DMSO 64 mg/mL (173.27 mM) and ethanol 64 mg/mL, water insoluble. The divergence between 36.9 mg/mL and >=100 mg/mL likely reflects differences in dissolution technique (sonication and warming versus vortexing alone), lot history, and the moisture sensitivity noted by Selleck. For stock preparation, Selleck's 10 mM recommendation in fresh anhydrous DMSO is the most conservative and reproducible starting point; sonication and warming to 37C may be required to reach the higher reported concentrations. A 70% ethanol / 30% propylene glycol vehicle has been cited for research use where an aqueous-free vehicle is desired. For in vivo formulation, MedChemExpress describes a vehicle of 10% DMSO -> 40% PEG300 -> 5% Tween-80 -> 45% saline achieving >=2.5 mg/mL (6.77 mM) as a clear solution, and Selleck lists a 5% DMSO / 40% PEG300 / 5% Tween-80 / 50% water vehicle at 3.700 mg/mL (10.02 mM). Prepare solutions fresh and aliquot; DMSO stocks should be stored under anhydrous conditions to prevent solubility loss.

Handling Precautions: Use powder-handling containment (glove box or fume hood with particulate control). Avoid inhalation of fine powder. Wear nitrile gloves, lab coat, and eye protection. RU-58841 is a research-grade anti-androgen; handle with the same institutional precautions applied to other endocrine-active research compounds. Selleck's technical note on DMSO stock precipitation in aqueous media recommends preheating the aqueous phase to 37C, mixing rapidly upon addition, and adding the aqueous phase last for complex vehicles.

Storage and Stability

Storage guidance for RU-58841 powder converges on -20C as the standard long-term condition, with desiccation and protection from light. MedChemExpress specifies 3 years at -20C and 2 years at 4C for powder, with DMSO solutions stable for 2 years at -80C or 1 year at -20C. Biozol lists a 1-year shelf life for its catalogue item. GLPBIO notes that stock solutions can be stored below -20C for several months and recommends warming to 37C with sonication to achieve higher solubility. Selleck recommends pre-aliquoting solid material rather than relying on long-term storage of stock solutions, because solid-state aliquots offer a longer shelf life than solutions. The principal storage consideration unique to RU-58841 among this catalogue's compounds is its sensitivity to moisture in DMSO: repeated opening of DMSO stock solutions can introduce water and reduce solubility, so aliquoting DMSO stocks into single-use fractions is preferable to repeated freeze-thaw cycles of a single stock.

Documentation Support

Per lot: COA, HPLC chromatogram, and mass spectrometry data. Where available from the supplier, NMR data, water content, and residual solvent data are provided. Custom specifications and third-party inspection can be arranged on a project basis.

About Knowlux

Knowlux Biotechnology is a GMP-oriented manufacturer and supplier of peptides, APIs and fine-chemical research compounds, operating from Hubei, China. We serve research groups, CDMOs and distributors in more than 40 countries, and support contract synthesis, custom packaging and technical documentation requests.

Compliance Statement

FOR RESEARCH USE ONLY. NOT FOR HUMAN USE. NOT FOR DIAGNOSTIC OR THERAPEUTIC USE.

This product is supplied for laboratory research use only. It is not for human or animal administration, not for diagnostic or therapeutic use, not for retail sale, and not for personal use. RU-58841 is not approved as a medicinal or cosmetic product in any jurisdiction. The purchaser is responsible for verifying product specifications against their specific research requirements and for compliance with all applicable institutional, local, and national regulations governing research chemical acquisition, storage, and use. Research context statements are for scientific reference only and do not constitute medical advice, promotional claims, or dosing guidance.

Data Verification Notes: The molecular formula C17H18F3N3O3 and molecular weight 369.34 are confirmed across MedChemExpress, Selleck, GLPBIO, ChemicalBook, ChemWhat, and CapotChem. The InvivoChem formula C17H18F3NO3 (one nitrogen fewer) is noted as a data entry error and not adopted. The IUPAC name and SMILES/InChIKey are from Selleck and MedChemExpress. Solubility values are reported with their source conditions rather than reconciled into a single figure because the DMSO measurements span 36.9 mg/mL to >=100 mg/mL and reflect differences in dissolution technique, lot history, and moisture sensitivity; Selleck's 10 mM stock recommendation in fresh anhydrous DMSO is presented as the most reproducible starting condition. Purity ranges are reported by supplier tier rather than as a single consensus value because RU-58841 lacks a compendial monograph and specifications are supplier-defined. The receptor pharmacology values (IC50 ~100 nM; ka 1.1 nM; BindingDB IC50 16 nM and 32 nM) are from BenchChem, Ambeed, and BindingDB and are assay-dependent. The in vivo topical selectivity data (1 microgram regression dose; no systemic anti-androgenic effect up to 100 micrograms) are from the 1994 European Journal of Endocrinology paper as cited in the search results.

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