5 alpha Reductase (5α-reductases), also known as 3-oxo-5α-steroid 4-dehydrogenases, are enzymes involved in steroid metabolism. They participate in 3 metabolic pathways: bile acid biosynthesis, androgen and estrogen metabolism, and prostate cancer.


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Metabolic Enzyme/Protease >
15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
Neuronal Signaling >
5-HT Receptor AChE Adenosine Kinase Amyloid-β Beta-secretase CaMK CGRP Receptor COMT Dopamine Receptor Dopamine Transporter FAAH GABA Receptor GlyT iGluR Imidazoline Receptor mAChR Melatonin Receptor Monoamine Oxidase nAChR Neurokinin Receptor Opioid Receptor Serotonin Transporter γ-secretase
NF-κB >
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Vitamin D Related >
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CGP-53153

CGP-53153 is a steroidal inhibitor of 5 alpha reductase with IC50s of 36 and 262 nM in rat and human prostatic tissue, respectively.

  • CAS Number: 149281-19-6
  • MF: C23H33N3O2
  • MW: 383.52700
  • Catalog: 5 alpha Reductase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Stigmasterol glucoside

Stigmasterol glucoside is a sterol isolated from P. urinaria with high antioxidant and anti-inflammatory activities[1], act as an inhibitor of 5α-reductase with an IC50 of 27.2 µM[2].

  • CAS Number: 19716-26-8
  • MF: C35H58O6
  • MW: 574.831
  • Catalog: 5 alpha Reductase
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 673.6±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 361.2±31.5 °C

Pedunculagin

Pedunculagin is a potent 5α-reductase type 1 inhibitor. Pedunculagin inhibits nitric oxide (NO), IL-6, IL-8 production. Pedunculagin decreases the protein expression of 5α-reductase. Pedunculagin shows anti-inflammatory activity[1].

  • CAS Number: 113866-64-1
  • MF: C34H24O22
  • MW: 784.54100
  • Catalog: 5 alpha Reductase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Finasteride-d9

Finasteride-d9 is deuterium labeled Finasteride. 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[1][2][3].

  • CAS Number: 1131342-85-2
  • MF: C23H27D9N2O2
  • MW: 381.60
  • Catalog: 5 alpha Reductase
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 576.6±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 177.4±30.3 °C

12-O-Methylcarnosic acid

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[1][2].

  • CAS Number: 62201-71-2
  • MF: C21H30O4
  • MW: 346.461
  • Catalog: 5 alpha Reductase
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 505.1±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 173.3±23.6 °C

LY191704

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[1][2].

  • CAS Number: 146117-78-4
  • MF: C14H16ClNO
  • MW: 249.73600
  • Catalog: 5 alpha Reductase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dutasteride-13C6

Dutasteride-13C6 is the 13C labeled Dutasteride[1]. 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[2].

  • CAS Number: 1217685-27-2
  • MF: C2113C6H30F6N2O2
  • MW: 534.49
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LAPISTERIDE

Lapisteride (CS 891) is an orally active 5α-reductase inhibitor. Lapisteride can be used in cancer research[1].

  • CAS Number: 142139-60-4
  • MF: C29H40N2O3
  • MW: 464.64000
  • Catalog: 5 alpha Reductase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Finasteride acetate

Finasteride (acetate) is an orally active testosterone 5-alpha-reductase inhibitor. Target: 5-alpha ReductaseApproved: 1992Finasteride (acetate) is the acetate salt of finasteride which is a synthetic 4-azasteroid antiandrogen compound, is a specific inhibitor of steroid Type II 5α-reductase, an intracellular enzyme that converts the androgen testosterone into 5α-dihydrotestosterone (DHT). Finasteride is used in the treatment of prostate cancer, benign prostatic hyperplasia, and androgenetic alopecia (male pattern baldness). In benign prostatic hyperplasia, finasteride inhibits 5alpha-reductase activity in epithelium for Ki of 10nM, significantly lower than in stroma (Ki = 33nM) [1].

  • CAS Number: 222989-99-3
  • MF: C25H40N2O4
  • MW: 432.596
  • Catalog: 5 alpha Reductase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MK 386

MK 386 (L-733692) is a selective 5-α-reductase I inhibitor, used for prostate cancer inhibition[1].

  • CAS Number: 158493-17-5
  • MF: C28H49NO
  • MW: 415.69
  • Catalog: 5 alpha Reductase
  • Density: 0.951g/cm3
  • Boiling Point: 505.2ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 203.9ºC

Epristeride

Epristeride is a novel 5α-reductase inhibor.

  • CAS Number: 119169-78-7
  • MF: C25H37NO3
  • MW: 399.56600
  • Catalog: 5 alpha Reductase
  • Density: 1.13g/cm3
  • Boiling Point: 596ºC at 760mmHg
  • Melting Point: 242-249°
  • Flash Point: 314.3ºC

MK-4541

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[1].

  • CAS Number: 796885-38-6
  • MF: C22H31F3N2O3
  • MW: 428.49
  • Catalog: 5 alpha Reductase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Finasteride

Finasteride is an orally active testosterone 5-alpha-reductase inhibitor (Ki= 10 nM). Target: 5-alpha ReductaseApproved: 1992Finasteride, a synthetic 4-azasteroid antiandrogen compound, is a specific inhibitor of steroid Type II 5α-reductase, an intracellular enzyme that converts the androgen testosterone into 5α-dihydrotestosterone (DHT). Finasteride is used in the treatment of prostate cancer, benign prostatic hyperplasia, and androgenetic alopecia (male pattern baldness). In benign prostatic hyperplasia, finasteride inhibits 5alpha-reductase activity in epithelium for Ki of 10 nM, significantly lower than in stroma (Ki = 33nM) [1].

  • CAS Number: 98319-26-7
  • MF: C23H36N2O2
  • MW: 372.544
  • Catalog: 5 alpha Reductase
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 576.6±50.0 °C at 760 mmHg
  • Melting Point: 253 °C
  • Flash Point: 177.4±30.3 °C

17alpha-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.

  • CAS Number: 57-91-0
  • MF: C18H24O2
  • MW: 272.382
  • Catalog: 5 alpha Reductase
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 445.9±45.0 °C at 760 mmHg
  • Melting Point: 176-180ºC(lit.)
  • Flash Point: 209.6±23.3 °C

Dutasteride

Dutasteride (GG745) is a potent inhibitor of both 5 alpha-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT.IC50 Value:Target: 5 alpha-reductasein vitro: Dutasteride inhibited (3)H-T conversion to (3)H-DHT and, as anticipated, inhibited T-induced secretion of PSA and proliferation. However the drug also inhibited DHT-induced PSA secretion and cell proliferation (IC(50) approximately 1 microM). Dutasteride competed for binding the LNCaP cell AR with an IC(50) approximately 1.5 microM. High concentrations of dutasteride (10-50 microM), but not finasteride, in steroid-free medium, resulted in enhanced cell death, possibly by apoptosis [1]. Dutasteride reduces cell viability and cell proliferation in both cell lines tested (androgen-responsive (LNCaP) and androgen-unresponsive (DU145) human prostate cancer (PCa)) [2].in vivo: GG745 has a terminal half-life of approximately 240 hr, and single doses of >10 mg decreased DHT levels significantly more than did single 5-mg doses of finasteride [3]. In placebo treated men without prostate cancer there was an 8.3% median increase in PSA at month 24 compared with -59.5% in those who received dutasteride, using doubled values to correct for dutasteride treatment [4].Toxicity: Dutasteride may affect male fertility and steroid hormone dynamics. Therefore, a 21-day reproduction study was conducted to determine the effects of dutasteride (10, 32 and 100 μg/L) on fish reproduction. Exposure to dutasteride significantly reduced fecundity of fish and affected several aspects of reproductive endocrine functions in both males and females [5].Clinical trial: Bioequivalence Study Of Dutasteride Five 0.1 mg And One 0.5 mg Soft Gelatin Capsules In Healthy Male Volunteers. Phase 1

  • CAS Number: 164656-23-9
  • MF: C27H30F6N2O2
  • MW: 528.530
  • Catalog: 5 alpha Reductase
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 620.3±55.0 °C at 760 mmHg
  • Melting Point: 242-250ºC
  • Flash Point: 329.0±31.5 °C