Tamoxifen 20mg

$28.00

Chemical Information and Compositions of Tamoxifen 20mg

For researchers, biochemists, and wholesale distributors, the molecular structure of Tamoxifen 20mg is fascinating. It belongs to the triphenylethylene class, sharing structural DNA with Clomiphene and Toremifene. Understanding its composition is vital for analytical testing, formulation, and predicting its biological behavior.

Official Chemical Nomenclature

  • Chemical Name: (Z)-2-[4-(1,2-diphenylbut-1-enyl)phenoxy]-N,N-dimethylethan-1-amine; 2-hydroxypropane-1,2,3-tricarboxylic acid
  • Chemical Formula: C32H37NO8 (as the Citrate salt)
  • Molecular Weight: 561.64 g/mol (as the Citrate salt). The base Tamoxifen has a molecular weight of 371.51 g/mol.
  • CAS Number: 54965-24-1 (Tamoxifen Citrate)

Structural Composition Breakdown

Tamoxifen 20mg is a triphenylethylene derivative. Its core structure features three phenyl rings attached to an ethylene bridge. The specific substitutions on this core dictate its SERM activity:

  1. The Z-Isomer (Trans-configuration): Tamoxifen exists as a mixture of Z (trans) and E (cis) isomers, but the pharmaceutical formulation is predominantly the Z-isomer, which is the active anti-estrogenic component.
  2. Basic Side Chain: The inclusion of a dimethylaminoethoxy side chain on the terminal phenyl ring is critical. This basic side chain is responsible for the compound’s anti-estrogenic activity. It allows Tamoxifen to bind competitively to the estrogen receptor and induce a conformational change that prevents the receptor from interacting with co-activators necessary for DNA transcription.
  3. Citrate Salt: To make the base Tamoxifen molecule (which is highly lipophilic and unmanageable as a solid) water-soluble and bioavailable for oral administration, it is formulated as a citrate salt.

Physical and Chemical Properties

  • State at Room Temperature: Solid (Fine Crystalline Powder)
  • Color: White to off-white
  • Solubility: Very slightly soluble in water (0.4 mg/mL); soluble in methanol, acetone, and DMSO; practically insoluble in ether.
  • Melting Point: Approximately 140°C to 142°C (with decomposition of the citrate salt).

Pharmacokinetics

  • Route of Administration: Oral
  • Absorption: Rapidly and well absorbed from the gastrointestinal tract.
  • Half-Life: Tamoxifen 20mg has a highly complex pharmacokinetic profile. The parent compound has a half-life of roughly 5 to 7 days. However, its primary active metabolite, Endoxifen, also has a long half-life. Due to this extensive half-life, steady-state plasma levels are not reached for approximately 4 weeks of daily dosing. This long half-life necessitates strategic loading doses in certain performance protocols.
  • Metabolism: Extensively metabolized in the liver primarily via the Cytochrome P450 enzyme system, particularly CYP3A4 and CYP2D6. CYP3A4 converts Tamoxifen into N-desmethyl Tamoxifen, which is then converted by CYP2D6 into Endoxifen. Endoxifen is 100 times more potent than the parent Tamoxifen compound at blocking the estrogen receptor.
  • Excretion: Primarily through the feces via biliary elimination, with a small fraction excreted in urine.

Formulation Details: The 20mg Pill

When you source wholesale Tamoxifen 20mg, you are purchasing the Citrate salt formulation. A 20mg pill contains 20mg of Tamoxifen (base equivalent), which equates to approximately 30.4mg of Tamoxifen Citrate. Standard excipients used in the tableting process include lactose, microcrystalline cellulose, croscarmellose sodium, and magnesium stearate. For B2B buyers, the geometric dilution of the active API with these excipients is critical to ensure uniform dosing in every single pill across massive batches.