NOLVADEX (Tamoxifen Citrate)
Tamoxifen citrate has a molecular weight of 563.62, the pKa’ is 8.85, the equilibrium solubility in water at 37°C is 0.5 mg/mL and in 0.02 N HCl at 37°C, it is 0.2 mg/mL.
CLINICAL PHARMACOLOGY NOLVADEX…
is a nonsteroidal agent that has demonstrated potent antiestrogenic properties in animal test systems.
The antiestrogenic effects may be related to its ability to compete with estrogen for binding sites in target tissues such as breast. Tamoxifen inhibits the induction of rat mammary carcinoma induced by dimethylbenzanthracene (DMBA) and causes the regression of already established DMBA-induced tumors. In this rat model, tamoxifen appears to exert its antitumor effects by binding the estrogen receptors. In cytosols derived from human breast adenocarcinomas, tamoxifen competes with estradiol for estrogen receptor protein.
Clomid’s method of action is actually quite simple to understand – just like all SERM’s, it prevents estrogen from binding to receptors, not allowing this hormone to reach the pituitary glands. This causes stimulation of LH (luteinizing hormone), and FSH (Follicle Stimulating Hormone), leading to a temporary spike in testosterone levels. Hence its popularity during post cycle therapy.
Human Chorionic Gonadotropin (HCG) is a polypeptide hormone created in both men and women. It is produced in large amounts during women’s pregnancy and men secrete it in large amounts during puberty. HCG stimulates the natural testosterone production system of men that present low levels of Luteinizing Hormone (LH) and Follicle-Stimulating Hormone (FSH).
HCG is composed of an alpha and a beta sub-unit. The alpha sub-unit is essentially identical to the alpha sub units of the human pituitary gonadotropins, luteinizing hormone (LH) and follicle-stimulating hormone (FSH), as well as to the alpha sub-unit of human thyroid-stimulating hormone (TSH), while the beta sub units of these hormones differ in amino acid sequence.
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