E-Control Rx 2.0™ contains Arimistane, also known as androsta-3,5-deine-7, 17 dione. Arimistane is a potent aromatase inhibitor to decrease circulating levels of estrogen in the body. Simply put, Arimistane will inhibit or reduce the amount of androgens in the body that can convert into estrogen. Arimistane is a suicide aromatase inhibitor, meaning that it binds to the aromatase enzyme, and can not be reversed.
Estrogen is a hormone that is made up of three different compounds, which are estrone, estradiol, and estriol. Estrogen is not only important for human development, but it contributes to the development of secondary sex characteristics. It determines the main characteristics of a man and a woman. Although, estrogen is important in human development, excess estrogen can lead to health risks including breast cancer, weight gain, headaches, and gynecomastia. Having too much or an imbalance of estrogen can negatively impact your performance in the gym. In order to maximize optimal environment for muscle growth and recovery, you want to maximize your body’s testosterone and luteinizing hormones (LH).
So how does Arimistane help with all this?
Arimistane has been developed as a natural metabolite of DHEA known as androsta-3,5-deine-7, 17 dione. Arimistane is a potent aromatase inhibitor to decrease circulating levels of estrogen in the body. Simply put, Arimistane will inhibit or reduce the amount of androgens in the body that can convert into estrogen. Arimistane is a suicide aromatase inhibitor, meaning that it binds to the aromatase enzyme, and can not be reversed. Past in vitro studies show that Arimistane compared to other aromatase inhibitors has a great binding affinity to the aromatase enzyme, which leads to greater effectiveness in shutting down the active of the aromatase enzyme. The binding affinity is measured in Ki value, which measures the how well the aromastase inhibitor binds to the aromatase enzyme. See graph below.
In measuring the effectiveness of the binding affinity to the enzymes, lower Ki value represents higher binding affinity.
Ki value of Arimistane is .22 micromolar (.mu.M)
Ki value of 3-OHAT (3-beta-hydroxyandrost-4-ene-6,17-dione) is 6.5 .mu.M
Ki value of AT (androst-4-ene-3,6,17-trione) commonly referred to as 6oxo is .43 .mu.M
Ki value of formestane (4-hydroxyandrost-4-ene-3,17-dione, 4-OHA, 16) is .6 .mu.M
Aromatase enzyme increases → estrogen
Arimastane decreases ↓estrogen
High estrogen in men will lower ↓LH (luteinizing hormones) in turn lower ↓testosterone
Conclusion: Arimastane = increased ↑LH and increase ↑testosterone
References: Numazawa M, Mutsumi A, Tachibana M, Hoshi K; Synthesis of androst-5-en-7-ones and androsta-3,5-dien-7-ones and their related 7-deoxy analogs as conformational and catalytic probes for the active site of aromatase; J Med Chem. 1994 Jul 8;37(14):2198-205
Burnett-Bowie SA, Roupenian KC, Dere ME, Lee H, Leder BZ. Effects of aromatase inhibition in hypogonadal older men: a randomized, double-blind, placebo-controlled trial. Clin Endocrinol (Oxf). 2008 Jun 25. [Epub ahead of print]
J. Raman, P. Schlegel Aromatase Inhibitors for Male Infertility The Journal of Urology, Volume 167, Issue 2, Pages 624-629.
Schubert K, Wehrberger K, Hobe G; Androsta-3,5-diene-7,17-dione: isolation from urine and formation from 7-keto-dehydro-epiandrosterone sulphate under various conditions of hydrolysis; Endocrinol Exp. 1971 Dec;5(4):205-10
Numazawa M, Tsuji M, Mutsumi A; Studies on aromatase inhibition with 4-androstene-3,6,17-trione: its 3 beta-rededuction and time-dependent irreversible binding to aromatase with human placental microsomes; J Steriod Biochem. 1987 Sep 28 (3): 337-44
Njar VC, Grun G, Hartmann RW; Evaluation of 6,7-aziridinyl steroids and related compounds as inhibitors of aromatase (P-450arom); J Enzyme Inhib. 1995; 9(3): 195-202
This product should only be used by healthy adults at least 21 years old. Do not exceed the recommended dose or duration. Do not use if you are at risk of, or being treated for diabetes, liver problems or high blood pressure. Do not drink alcohol while using this product, and increase daily water intake. This product can negatively affect male fertility. Always Consult your health care professional before using any dietary supplements.
As a dietary supplement, take one (1) capsule three (3) times daily in divided doses per day, with food.
Use in cycles of 4 to 6 weeks taking at least 2 to 4 weeks off in between cycles.
Do not exceed the recommended dose or duration. This product should only be used by healthy adults at least 21 years old. Do no use if pregnant or nursing, or if you are at risk of, or being treated for diabetes, liver problems or high blood pressure. Consult your health care professional before using any dietary supplements.