RAD-140 (Testolone)

$30.00

Chemical Information and Compositions of RAD-140

For researchers, biochemists, and wholesale distributors, the molecular structure of RAD-140 is a triumph of modern medicinal chemistry. Understanding its composition is vital for analytical testing, formulation, and predicting its biological behavior.

Official Chemical Nomenclature

  • IUPAC Name: 2-chloro-4-[[(1R,2S)-1-hydroxy-2-methyl-1-propan-2-ylcyclopropyl]carbamoyl]-2-methyl-N-[4-cyano-3-(trifluoromethyl)phenyl]benzamide
  • Chemical Formula: C20H16ClF3N3O3 (Note: some older literature cites C20H16ClN5O2 based on a nitrile isomer, but the standard synthesized API formula is C20H16ClF3N3O3)
  • Molecular Weight: 434.32 g/mol
  • CAS Number: 1182367-47-0

Structural Composition Breakdown

RAD-140 is a non-steroidal ligand. Its structural architecture is precisely tailored to exploit the shape of the androgen receptor (AR) ligand-binding domain (LBD):

  1. The Trifluoromethylphenyl Moiety: The inclusion of a trifluoromethyl (-CF3) group on the distal phenyl ring is a classic optimization. The high electronegativity and lipophilicity of the fluorine atoms increase the molecule’s metabolic stability and membrane permeability, preventing rapid hepatic destruction.
  2. The Cyanophenyl Group: A nitrile (cyano) group attached to the phenyl ring is critical for hydrogen bonding with specific amino acid residues (like Asn705 and Gln711) in the AR, anchoring the molecule securely.
  3. The Chlorobenzamide Core: The chloro-substituted benzamide ring provides conformational rigidity. This rigidity ensures RAD-140 maintains a specific spatial orientation that perfectly matches the AR’s active site, driving its exceptionally high binding affinity.
  4. The Hydroxycyclopropyl Group: The chiral 1-hydroxy-2-methylcyclopropyl group is the defining structural signature of RAD-140. This bulky, three-dimensional group mimics the C/D ring system of natural steroids. It physically blocks co-activator proteins from binding to the AR in certain tissues (like the prostate), which is the fundamental mechanism of its tissue selectivity.

Physical and Chemical Properties

  • State at Room Temperature: Solid (Crystalline Powder)
  • Color: White to off-white
  • Solubility: Practically insoluble in water; soluble in DMSO, PEG 400, ethanol, and methanol. Its poor aqueous solubility necessitates specific excipient matrices for oral capsule formulation.
  • Melting Point: Approximately 115°C to 120°C.

Pharmacokinetics

  • Route of Administration: Oral
  • Absorption: Rapidly and well absorbed from the gastrointestinal tract.
  • Half-Life: The terminal elimination half-life of RAD-140 in humans is estimated to be 60 hours (roughly 2.5 days). This exceptionally long half-life allows for stable blood plasma levels with once-daily dosing, but it also means the compound takes weeks to clear the system, prolonging suppression and requiring careful PCT planning.
  • Metabolism: Primarily metabolized in the liver via CYP3A4, but it lacks the 17-alpha-alkylation of oral steroids, sparing it from severe hepatotoxic first-pass effects.
  • Excretion: Excreted primarily via the feces through biliary elimination, with a minor renal fraction.

Formulation Details: The Capsule

When you source wholesale RAD-140, you are dealing with a micro-dose formulation. Standard research doses range from 10mg to 20mg daily.

A 10mg dose equals 0.010 grams. Standard excipients used in the encapsulation process include:

  • Microcrystalline Cellulose (MCC): Filler to provide bulk.
  • Magnesium Stearate: Lubricant for encapsulation flow.
  • Hypromellose (HPMC): For vegetarian capsule shells.

For B2B buyers, ensuring the uniform blending of such a microscopic amount of API within the excipient matrix via geometric dilution is critical. Because RAD-140 is highly suppressive, “hot spots” (capsules containing 30mg+) in a poorly blended batch can cause immediate, severe HPTA shutdown and estrogen crashes.

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