5 alpha Reductase 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.

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.

Epristeride-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 K_i value of 0.7-2 nM. Epristeride can be used for the research of prostatic hyperplasia and acne.

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.

Gestodene-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.

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.

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.

Gestodene-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.

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.

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.

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.

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.

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).

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.

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.

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.

(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.

SRD5A1-IN-2 is a inhibitor of steroid 5α-reductase type-1 (SRD5A1), with an IC₅₀ of 8.5 μM. SRD5A1-IN-2 downregulates SRD5A1 protein expression in HaCaT cells. SRD5A1-IN-2 reduces dihydrotestosterone (DHT) production in HaCaT cells. SRD5A1-IN-2 can be used for the study of androgen-related conditions such as androgenetic alopecia (AGA).

Turosteride is a selective 5 alpha-reductase inhibitor, with IC₅₀ values of 55 and 53 nM for human and rat prostatic 5 alpha-reductases, respectively. Turosteride can reduce the prostate and seminal vesicle weights.

MK-0434 is an orally active steroid 5α-reductase inhibitor. MK-0434 specifically inhibits steroid 5α-reductase, thereby reducing the level of dihydrotestosterone (DHT) in the body. MK-0434 can be used in the study of benign prostatic hyperplasia.