1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. 5 alpha Reductase

5 alpha Reductase

5α-reductase

Steroid 5-α reductase (5AR) is a membrane-bound protein that is responsible for reducing steroids such as testosterone, progesterone, and androstenedione to 5-α reduced metabolites such as 5-α dihydrotestosterone (DHT), 5-α dihydroprogesterone and androstanedione, respectively. There are three isoforms of 5AR in humans: SRD5A1, SRD5A2, and SRD5A3. SRD5A1 and SRD5A2 have functionality for 5-α reduction of steroids in humans. DHT is a more potent androgen than testosterone and has a function in androgen receptor activation.

The inactivating mutations in 5αR2 lead to disorders of sexual development. The regulation of 5AR is important for the treatment of benign prostate hyperplasia (BPH) and prostate cancer (PC), and 5AR inhibitors are widely used for the treatment of androgen-dependent benign or malignant prostatic diseases.

5 alpha Reductase Related Products (48):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-106129
    Izonsteride
    Inhibitor
    Izonsteride (Compound LY320236) is an inhibitor of 5α-reductase (IC50 = 11.6 nM for type I; 7.37 nM for type II). LY320236 inhibits the activity of steroid 5α-reductase, preventing the conversion of testosterone (T) to dihydrotestosterone (DHT). LY320236 can significantly inhibit the growth of LNCaP tumors in thymic mice without exhibiting obvious host toxicity.
    Izonsteride
  • HY-N7510R
    12-O-Methylcarnosic acid (Standard)
    Inhibitor
    12-O-Methylcarnosic acid (Standard) is the analytical standard of 12-O-Methylcarnosic acid. This product is intended for research and analytical applications. 12-O-Methylcarnosic acid (12-Methoxycarnosic acid), a diterpene carnosic acid isolated from the acetone extract of Salvia microphylla, is an active constituent of 5α-reductase inhibition with an IC50 value of 61.7 μM. 12-O-Methylcarnosic acid inhibits proliferation in LNCaP cells. 12-O-Methylcarnosic acid has antioxidant, anti-cancer and antimicrobial activity.
    12-O-Methylcarnosic acid (Standard)
  • HY-118091B
    LY300503
    Control
    LY300503 is an enantiomer of LY191704. LY191704 is a human type I 5α-reductase inhibitor.
    LY300503
  • HY-106951
    MK 386
    MK 386 (L-733692) is a selective 5-α-reductase I inhibitor, used for prostate cancer inhibition.
    MK 386
  • HY-106614
    Osaterone acetate
    Inhibitor
    Osaterone acetate is an orally active steroid anti-androgen agent, mainly used for benign prostatic hyperplasia (BPH) in dogs. Osaterone acetate competitively antagonizes androgen receptor and inhibits 5α-reductase, reducing the concentration of dihydrotestosterone (DHT) while blocking the growth-stimulating effects of testosterone and DHT on prostate cells. Osaterone acetate can rapidly alleviate the symptoms of BPH in dogs without affecting the fertility of breeding dogs.
    Osaterone acetate
  • HY-133949
    8,11-Eicosadiynoic acid
    Inhibitor
    8,11-Eicosadiynoic acid, an unsaturated fatty acid, is a steroid 5α-reductase inhibitor. 8,11-Eicosadiynoic acid can be used for the research of acne.
    8,11-Eicosadiynoic acid
  • HY-118091A
    Bexlosteride
    Inhibitor
    Bexlosteride (LY300502) is a benzoquinolinone human type I 5α-reductase inhibitor. Bexlosteride shows metabolic inhibitory, antiproliferative, and antisecretory effects in LNCaP human prostatic adenocarcinoma cell cultures. Bexlosteride can be used for the research of prostatic cancer.
    Bexlosteride
  • HY-13613S
    Dutasteride-13C6
    Dutasteride-13C6 is the 13C labeled Dutasteride. Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT.
    Dutasteride-<sup>13</sup>C<sub>6</sub>
  • HY-125065
    MK-4541
    Antagonist
    MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model.
    MK-4541
  • HY-13613S2
    Dutasteride-13C,15N,d
    Inhibitor
    Dutasteride-13C,15N,d is 15N and deuterated labeled Dutasteride (HY-13613). Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT.
    Dutasteride-<sup>13</sup>C,<sup>15</sup>N,d
  • HY-13635R
    Finasteride (Standard)
    Inhibitor
    Finasteride (Standard) is the analytical standard of Finasteride. This product is intended for research and analytical applications. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia.
    Finasteride (Standard)
  • HY-19292
    AS-601811
    Inhibitor
    AS-601811(compound 47) is a 5alpha-reductase 1 inhibitor with the IC50 of 20 nM and can be used for study of alopecia and hirsutism.
    AS-601811
  • HY-19144
    ONO-3805
    Inhibitor
    ONO-3805 is an early lead compound of a non-steroidal 5α-reductase inhibitor, used to inhibit the conversion of testosterone to dihydrotestosterone, with potential effects in inhibiting benign prostatic hyperplasia.
    ONO-3805
  • HY-118091
    LY191704
    Inhibitor
    LY191704, as a benzoquinolinone, is a potent, nonsteroidal, noncompetitive and selective human type I 5α-reductase inhibitor. LY191704 is a racemic mixture of the compounds LY300502 and LY300503. LY191704 may be useful in the research of human endocrine disorders associated with overproduction of dihydrotestosterone (DHT) by 5α-reductase type 1.
    LY191704
  • HY-165478
    FCE 28260
    Inhibitor
    FCE 28260 is an orally active 4-azacyclic 5α-reductase (5αR) inhibitor. FCE 28260 exhibits IC₅₀ values for human 5αR type 1 and 5αR type 2 of 36 and 3.3 nM, respectively, and for human and rat prostates with IC₅₀ values of 16 and 15 nM, respectively. FCE 28260 simultaneously blocks the production of dihydrotestosterone (DHT) in the prostate and peripheral tissues. FCE 28260 can significantly inhibit the induction of prostatic and seminal vesicle hyperplasia by testosterone (T) in rat models, without inhibiting the growth of the prostate in DHT implantation models. FCE 28260 can be used for the studies DHT-dependent diseases such as benign prostatic hyperplasia (BPH).
    FCE 28260
  • HY-121700
    L-751788
    Inhibitor
    L-751788 is a selective inhibitor of type I of 5α-reductase. L-751788 does not have a significant impact on the differentiation of the external genitalia in animals. When administered orally to pregnant rhesus monkeys, L-751788 (2, 10 mg/kg) did not cause abnormalities in fetal external genitalia.
    L-751788
  • HY-165595
    Glutamic acid-alanine-glycine mixture
    Activator
    The glutamic acid-alanine-glycine mixture is an orally active activator of testosterone 5α-reductase (5α-reductase). It promotes prostate function by enhancing the activity of 5α-reductase and increasing the levels of free amino acids. However, when combined with testosterone and estradiol (HY-B0141R), the glutamic acid-alanine-glycine mixture inhibits 5α-reductase activity and decreases the levels of free amino acids. The glutamic acid-alanine-glycine mixture can be used in research related to prostate function and endocrine disorders.
    Glutamic acid-alanine-glycine mixture
  • HY-13635A
    Finasteride acetate
    Inhibitor
    Finasteride (MK-906) acetate is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride acetate has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride acetate can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia.
    Finasteride acetate
  • HY-B1734
    16-Dehydropregnenolone acetate
    Inhibitor
    16-Dehydropregnenolone acetate (16-DPA), a sterols compound, is an orally active 17α-hydroxylase and 5α-reductase inhibitor. 16-Dehydropregnenolone is also a potent bile acid receptor (BAR)/farnesoid X receptor (FXR) antagonist. 16-Dehydropregnenolone hypolipidemic and anticancer effects. 16-Dehydropregnenolone acetate (16-DPA) is the drug intermediate that can be used for synthesis of Dexamethasone (HY-14648) and related other steroidal pharmacophores.
    16-Dehydropregnenolone acetate
  • HY-N13195
    (15α)-15,26-Dihydroxylanosta-7,9(11),24-trien-3-one
    Inhibitor
    (15α)-15,26-Dihydroxylanosta-7,9(11),24-trien-3-one shows a 5a-reductase inhibitory activity with an IC50 value of 41.9 μM. (15α)-15,26-Dihydroxylanosta-7,9(11),24-trien-3-one inhibits the growth of the ventral prostate induced by testosterone in rat. (15α)-15,26-Dihydroxylanosta-7,9(11),24-trien-3-one is promising for research of benign prostatic hyperplasia (BPH) as well as other 5α-dihydrotestosterone (DHT)-related disorders, such as acne and male pattern baldness.
    (15α)-15,26-Dihydroxylanosta-7,9(11),24-trien-3-one