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.
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5 alpha Reductase Related Products (53)
Related Products (53)
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Alpha-Estradiol-d3
0 ImagesCat. No.: HY-B0141ASSynonyms: Alfatradiol-d3; Epiestradiol-d3; Epiestrol-d3Alpha-Estradiol-d3 is the deuterium labeled Alpha-Estradiol. Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
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Izonsteride
0 ImagesCat. No.: HY-106129CAS No.: 176975-26-1Synonyms: LY 320236Izonsteride (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.
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12-O-Methylcarnosic acid (Standard)
0 ImagesCat. No.: HY-N7510RCAS No.: 62201-71-2Synonyms: 12-Methoxycarnosic acid (Standard)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.
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LY300503
0 ImagesCat. No.: HY-118091BCAS No.: 148905-79-7LY300503 is an enantiomer of LY191704. LY191704 is a human type I 5α-reductase inhibitor.
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MK 386
0 ImagesCat. No.: HY-106951CAS No.: 158493-17-5Synonyms: L-733692MK 386 (L-733692) is a selective 5-α-reductase I inhibitor, used for prostate cancer inhibition.
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Osaterone acetate
0 ImagesCat. No.: HY-106614CAS No.: 105149-00-6Osaterone 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.
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8,11-Eicosadiynoic acid
0 ImagesCat. No.: HY-133949CAS No.: 82073-91-48,11-Eicosadiynoic acid, an unsaturated fatty acid, is a steroid 5α-reductase inhibitor. 8,11-Eicosadiynoic acid can be used for the research of acne.
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Epristeride-d9
0 ImagesCat. No.: HY-107385SSynonyms: ONO-9302-d9; SKF105657-d9Epristeride-d9 (ONO-9302-d9) is the deuterium labeled Epristeride (HY-107385). Epristeride (ONO-9302) is a selective, specific and orally active uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2. Epristeride has inhibitory effects for SR isoenzymes types 2 with Ki value of 0.7-2 nM. Epristeride can be used for the research of prostatic hyperplasia and acne.
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Bexlosteride
0 ImagesCat. No.: HY-118091ACAS No.: 148905-78-6Synonyms: LY300502Bexlosteride (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.
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Dutasteride-13C6
0 ImagesCat. No.: HY-13613SCAS No.: 1217685-27-2Synonyms: GG 745-13C6; GI 198745-13C6Dutasteride-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.
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Gestodene-d7
0 ImagesCat. No.: HY-W753897Synonyms: SHB 331-d7; WL 70-d7Gestodene-d7 (SHB 331-d7; WL 70-d7) is the deuterated-labeled Gestodene (HY-B0110). Gestodene is an orally active synthetic progestogen compound of the 19-nortestosterone class. Gestodene binds with high affinity to the progesterone receptor, inhibits 5α-reductase, binds to androgen and aldosterone receptors, and inactivates CYP3A. Gestodene acts as a positive allosteric modulator of PAR1, enhances PAR1-mediated signaling pathways, and is capable of increasing the activation potency of PAR1-AP toward PAR1, thereby promoting ERK1/2 phosphorylation, receptor internalization, cell morphological changes, and human platelet aggregation. Gestodene and its A-ring reduced metabolites promote the proliferation, differentiation, and mineralization of neonatal rat osteoblasts. Gestodene itself has no binding capacity for estrogen receptors, and this osteogenic activity depends on intracellular metabolism to generate A-ring reduced products with estrogen-like agonistic activity. Gestodene is useful for research on diseases related to progesterone secretion and diseases related to thrombosis.
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MK-4541
0 ImagesCat. No.: HY-125065CAS No.: 796885-38-6MK-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.
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Dutasteride-13C,15N,d
0 ImagesCat. No.: HY-13613S2Synonyms: GG 745-13C,15N,d; GI 198745-13C,15N,dDutasteride-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.
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Finasteride (Standard)
0 ImagesSynonyms: MK-906 (Standard)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.
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Gestodene-d6
0 ImagesCat. No.: HY-B0110SCAS No.: 1542211-40-4Synonyms: SHB 331-d6; WL 70-d6Gestodene-d6 (SHB 331-d6; WL 70-d6) is the deuterated-labeled Gestodene (HY-B0110). Gestodene is an orally active synthetic progestogen compound of the 19-nortestosterone class. Gestodene binds with high affinity to the progesterone receptor, inhibits 5α-reductase, binds to androgen and aldosterone receptors, and inactivates CYP3A. Gestodene acts as a positive allosteric modulator of PAR1, enhances PAR1-mediated signaling pathways, and is capable of increasing the activation potency of PAR1-AP toward PAR1, thereby promoting ERK1/2 phosphorylation, receptor internalization, cell morphological changes, and human platelet aggregation. Gestodene and its A-ring reduced metabolites promote the proliferation, differentiation, and mineralization of neonatal rat osteoblasts. Gestodene itself has no binding capacity for estrogen receptors, and this osteogenic activity depends on intracellular metabolism to generate A-ring reduced products with estrogen-like agonistic activity. Gestodene is useful for research on diseases related to progesterone secretion and diseases related to thrombosis.
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AS-601811
0 ImagesCat. No.: HY-19292CAS No.: 194979-95-8AS-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.
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ONO-3805
0 ImagesCat. No.: HY-19144CAS No.: 119347-91-0ONO-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.
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LY191704
0 ImagesCat. No.: HY-118091CAS No.: 146117-78-4LY191704, 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.
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Gestodene (Standard)
0 ImagesCat. No.: HY-B0110RCAS No.: 60282-87-3Synonyms: SHB 331 (Standard); WL 70 (Standard)Gestodene (Standard) (SHB 331 (Standard); WL 70 (Standard)) is the analytical standard of Gestodene (HY-B0110). This product is intended for research and analytical applications. Gestodene is an orally active synthetic progestogen compound of the 19-nortestosterone class. Gestodene binds with high affinity to the progesterone receptor, inhibits 5α-reductase, binds to androgen and aldosterone receptors, and inactivates CYP3A. Gestodene acts as a positive allosteric modulator of PAR1, enhances PAR1-mediated signaling pathways, and is capable of increasing the activation potency of PAR1-AP toward PAR1, thereby promoting ERK1/2 phosphorylation, receptor internalization, cell morphological changes, and human platelet aggregation. Gestodene and its A-ring reduced metabolites promote the proliferation, differentiation, and mineralization of neonatal rat osteoblasts. Gestodene itself has no binding capacity for estrogen receptors, and this osteogenic activity depends on intracellular metabolism to generate A-ring reduced products with estrogen-like agonistic activity. Gestodene is useful for research on diseases related to progesterone secretion and diseases related to thrombosis.
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FCE 28260
0 ImagesCat. No.: HY-165478CAS No.: 155651-56-2FCE 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).
