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Cl-4AS-1
Cl-4AS-1 is a dual anabolic–androgenic steroid (AAS) and 5α-reductase inhibitor. It is a potent and selective full agonist of the androgen receptor ( IC50 = 12 nM) and inhibitor of 5α-reductase 5α-Reductases, also known as 3-oxo-5α-steroid 4-dehydrogenases, are enzymes involved in steroid metabolism. They participate in three metabolic pathways: bile acid biosynthesis, androgen and estrogen metabolism. There are three isozymes of ... types I and II (IC50 = 6 and 10 nM, respectively). Structurally, Cl-4AS-1 is a 4-azasteroid. See also * TFM-4AS-1 References External links Cl-4AS-1 - Santa Cruz Biotechnology 5α-Reductase inhibitors Anabolic–androgenic steroids Androstanes Carboxamides Chloroarenes Lactams {{genito-urinary-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TFM-4AS-1
TFM-4AS-1 is a dual selective androgen receptor modulator (SARM) and 5α-reductase inhibitor. It is a potent and selective partial agonist ( Emax = 55%) of the androgen receptor ( IC50 = 30nM) and inhibitor of 5α-reductase types I and II (IC50 = 2 and 3 nM, respectively). TFM-4AS-1 shows tissue-selective androgenic effects; it promotes the accumulation of bone and muscle mass and has reduced effects in reproductive tissues and sebaceous glands. In an animal study, TFM-4AS-1 stimulated sebaceous gland formation only 31% as much as dihydrotestosterone Dihydrotestosterone (DHT, 5α-dihydrotestosterone, 5α-DHT, androstanolone or stanolone) is an endogenous androgen sex steroid and hormone. The enzyme 5α-reductase catalyzes the formation of DHT from testosterone in certain tissues includ ... (DHT) at doses that were as anabolic or more so than DHT. In addition, TFM-4AS-1 only weakly promoted growth of the prostate gland and it partially antagonized the actions of D ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anabolic–androgenic Steroid
Anabolic steroids, also known more properly as anabolic–androgenic steroids (AAS), are steroidal androgens that include natural androgens like testosterone as well as synthetic androgens that are structurally related and have similar effects to testosterone. They increase protein within cells, especially in skeletal muscles, and also have varying degrees of virilizing effects, including induction of the development and maintenance of masculine secondary sexual characteristics such as the growth of facial and body hair. The word ''anabolic'', referring to anabolism, comes from the Greek ἀναβολή ''anabole'', "that which is thrown up, mound". Androgens or AAS are one of three types of sex hormone agonists, the others being estrogens like estradiol and progestogens like progesterone. AAS were synthesized in the 1930s, and are now used therapeutically in medicine to stimulate muscle growth and appetite, induce male puberty and treat chronic wasting conditions, such as ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SRD5A2
The human gene ''SRD5A2'' encodes the 3-oxo-5α-steroid 4-dehydrogenase 2 enzyme, also known as 5α-reductase type 2 (5αR2), one of three isozymes of 5α-reductase. 5αR2 catalyzes the conversion of the male sex hormone testosterone into the more potent androgen, dihydrotestosterone. 5αR2 is a microsomal protein expressed at high levels in androgen-sensitive tissues such as the prostate. The enzyme is active at acidic pH and is sensitive to the 4-azasteroid inhibitor finasteride. Deficiencies in 5αR2 activity of the can lead to a condition known as 5α-reductase 2 deficiency, which is a cause of 46,XY DSD that presents as atypical male genitalia. See also * 5α-Reductase 5α-Reductases, also known as 3-oxo-5α-steroid 4-dehydrogenases, are enzymes involved in steroid metabolism. They participate in three metabolic pathways: bile acid biosynthesis, androgen and estrogen metabolism. There are three isozymes ... References Further reading * * * * * * * * * * * ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Androstanes
An androgen (from Greek ''andr-'', the stem of the word meaning "man") is any natural or synthetic steroid hormone that regulates the development and maintenance of male characteristics in vertebrates by binding to androgen receptors. This includes the embryological development of the primary male sex organs, and the development of male secondary sex characteristics at puberty. Androgens are synthesized in the testes, the ovaries, and the adrenal glands. Androgens increase in both males and females during puberty. The major androgen in males is testosterone. Dihydrotestosterone (DHT) and androstenedione are of equal importance in male development. DHT ''in utero'' causes differentiation of the penis, scrotum and prostate. In adulthood, DHT contributes to balding, prostate growth, and sebaceous gland activity. Although androgens are commonly thought of only as male sex hormones, females also have them, but at lower levels: they function in libido and sexual arousal. Also, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5α-Reductase Inhibitors
5α-Reductases, also known as 3-oxo-5α-steroid 4-dehydrogenases, are enzymes involved in steroid metabolism. They participate in three metabolic pathways: bile acid biosynthesis, androgen and estrogen metabolism. There are three isozymes of 5α-reductase encoded by the genes SRD5A1, SRD5A2, and SRD5A3. 5α-Reductases catalyze the following generalized chemical reaction: :a 3-oxo-5α-steroid + acceptor a 3-oxo-Δ4-steroid + reduced acceptor Where a 3-oxo-5α-steroid and acceptor are substrates, and a corresponding 3-oxo-Δ4-steroid and the reduced acceptor are products. An instance of this generalized reaction that 5α-reductase type 2 catalyzes is: :dihydrotestosterone + NADP+ \rightleftharpoons testosterone + NADPH + H+ where dihydrotestosterone is the 3-oxo-5α-steroid, NADP+ is the acceptor and testosterone is the 3-oxo-Δ4-steroid and NADPH the reduced acceptor. Production and activity The enzyme is produced in many tissues in both males and females, in the re ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
4-azasteroid
An azasteroid is a type of steroid derivative which has one of the carbon atoms in the steroid ring system replaced by a nitrogen atom. Two azasteroids, finasteride and dutasteride, are used clinically as 5α-reductase inhibitor 5α-Reductases, also known as 3-oxo-5α-steroid 4-dehydrogenases, are enzymes involved in steroid metabolism. They participate in three metabolic pathways: bile acid biosynthesis, androgen and estrogen metabolism. There are three isozymes of ...s. Some of the 6-azasteroids may prove to be useful drugs, but have yet to reach the pharmaceutical market. References Steroids {{pharmacology-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SRD5A1
3-Oxo-5α-steroid 4-dehydrogenase 1 is an enzyme that in humans is encoded by the ''SRD5A1'' gene. It is one of three forms of steroid 5α-reductase. Steroid 5α-reductase (EC 1.3.99.5) catalyzes, among other reactions, the conversion of testosterone into the more potent androgen, 5α-dihydrotestosterone (DHT). The ''SRD5A1'', ''SRD5A2'', and ''SRD5A3'' genes in humans all encode 5α-reductase isozymes. Function The 3-oxo-5α-steroid 4-dehydrogenase 1 enzyme is involved in bile acid biosynthesis, androgen and estrogen metabolism. For instance, the enzyme catalyzes the conversion of testosterone into the more potent androgen, 5α-dihydrotestosterone. It can also catalyze the conversion of progesterone, corticosterone or other steroids, to its corresponding 5α-3-oxo-steroids. This chemical reaction is called 5α-reduction, i.e. the reduction of the Δ5-4 double bond in steroids by catalyzing direct hydride transfer from NADPH to the carbon 5 position of the steroid subs ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5α-reductase Inhibitor
5α-Reductases, also known as 3-oxo-5α-steroid 4-dehydrogenases, are enzymes involved in steroid metabolism. They participate in three metabolic pathways: bile acid biosynthesis, androgen and estrogen metabolism. There are three isozymes of 5α-reductase encoded by the genes SRD5A1, SRD5A2, and SRD5A3. 5α-Reductases catalyze the following generalized chemical reaction: :a 3-oxo-5α-steroid + acceptor a 3-oxo-Δ4-steroid + reduced acceptor Where a 3-oxo-5α-steroid and acceptor are substrates, and a corresponding 3-oxo-Δ4-steroid and the reduced acceptor are products. An instance of this generalized reaction that 5α-reductase type 2 catalyzes is: :dihydrotestosterone + NADP+ \rightleftharpoons testosterone + NADPH + H+ where dihydrotestosterone is the 3-oxo-5α-steroid, NADP+ is the acceptor and testosterone is the 3-oxo-Δ4-steroid and NADPH the reduced acceptor. Production and activity The enzyme is produced in many tissues in both males and females, in the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enzyme Inhibitor
An enzyme inhibitor is a molecule that binds to an enzyme and blocks its activity. Enzymes are proteins that speed up chemical reactions necessary for life, in which substrate molecules are converted into products. An enzyme facilitates a specific chemical reaction by binding the substrate to its active site, a specialized area on the enzyme that accelerates the most difficult step of the reaction. An enzyme inhibitor stops ("inhibits") this process, either by binding to the enzyme's active site (thus preventing the substrate itself from binding) or by binding to another site on the enzyme such that the enzyme's catalysis of the reaction is blocked. Enzyme inhibitors may bind reversibly or irreversibly. Irreversible inhibitors form a chemical bond with the enzyme such that the enzyme is inhibited until the chemical bond is broken. By contrast, reversible inhibitors bind non-covalently and may spontaneously leave the enzyme, allowing the enzyme to resume its function. Rev ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
