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RAD-140 (Testolone), (10mg/capsule) 60 Capsules

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RAD-140 (Testolone) is a non-steroidal selective androgen receptor modulator (SARM) of the oxadiazole class, engineered for high-affinity, tissue-selective AR interaction. Radioligand competition assays confirm low-nanomolar Ki for AR, with functional selectivity characterised by differential co-regulator recruitment across tissue types in vitro. Research applications include AR structure–activity relationship studies, tissue-selective transcriptional activation profiling, and androgenic signalling pathway investigation.

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3D Molecular Structure

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Chemical Formula C20H16ClN5O2
Synonyms 2-chloro-4-(((1R,2S)-1-(5-(4-cyanophenyl)-1,3,4-oxadiazol-2-yl)-2-hydroxypropyl)amino)-3-methylbenzonitrile, RAD 140, Testolone
Molar Mass 393.8 g/mol
CAS Number 1182367-47-0
PubChem CID 44200882
Total Compound Content 600 mg (10 mg per capsule)
Shelf Life 36 months
RAD-140 is a non-steroidal selective androgen receptor modulator (SARM) of the oxadiazole class characterized by high-affinity androgen receptor (AR) binding in the low-nanomolar range. In vitro transactivation assays demonstrate potent AR-mediated transcriptional activity together with ligand-specific co-regulator recruitment patterns, a pharmacological profile that distinguishes RAD-140 from steroidal AR ligands and contributes to its utility in androgen receptor research. The compound lacks a steroid backbone and induces distinct receptor conformations that influence downstream transcriptional responses, making it a valuable tool for investigating AR signaling mechanisms and ligand-dependent receptor behavior. Metabolic characterization indicates oxidative biotransformation followed by conjugation pathways, with clearance profiles documented in experimental systems. Research applications include androgen receptor pharmacology, receptor-coregulator interaction mapping, androgen response element (ARE) activation studies, structure-activity relationship investigations, and comparative analyses of selective androgen receptor modulators. Supplied in 10 mg capsules. Independently third-party HPLC-tested; COA available per batch.

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How does RAD-140 differ from steroidal androgen receptor ligands in receptor pharmacology research?

RAD-140 is a non-steroidal androgen receptor modulator that binds AR with high affinity while inducing ligand-specific receptor conformations distinct from those produced by steroidal ligands. These conformational differences influence co-regulator recruitment, transcriptional activity, and downstream signaling behavior, making RAD-140 a valuable tool for investigating selective androgen receptor modulation and ligand-dependent receptor dynamics.

Q: What is the half-life of RAD-140 and how is it metabolized?

Pharmacokinetic investigations report an elimination half-life of approximately 60 hours. Metabolic characterization indicates oxidative biotransformation followed by conjugation pathways, with CYP-mediated metabolism contributing to compound clearance. Elimination profiles have been documented in experimental systems through both biliary and renal pathways.

Why is RAD-140 commonly used in androgen receptor signaling research?

RAD-140 combines high-affinity androgen receptor binding with a well-characterized pharmacological profile, making it useful for studies examining receptor activation mechanisms, co-regulator interactions, androgen response element (ARE) signaling, and structure-activity relationships. Its non-steroidal scaffold also makes it a valuable comparator in investigations of ligand-dependent androgen receptor behavior and selective receptor modulation.

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