Reductase

Aldose reductase-IN-1 (AT-001, Caficrestat) is a highly potent inhibitor of aldose reductase with an IC50 value of 28.9 pM, which can target the relaxin hormone signaling pathway in prostate cancer models.

Epristeride (ONO-9302) is an orally active, selective and non-competitive steroidal 5-α-reductase isoform 2 inhibitor that inhibits SR isoform 2.Episteride reduces prostate size and improves symptoms in men with BPH.Episteride induces atrophy and apoptosis of the ventral prostate in rats.

Alconil (Al 1567) is an aldose reductase inhibitor that may be used to study chronic obstructive pulmonary disease (COPD) and diabetes.

Sorbinil is an Aldose reductase inhibitor. Sorbinil plays a therapeutic role in treating diabetes and diabetic complications decreases AR activity and inhibit the polyol pathway.

MK 0434 is an orally active steroidal 5 alpha-reductase inhibitor.

Ginsenoside Ro (Chikusetsusaponin V) can reduce TXA2 production, weakly reduce COX-1 and TXAS activities, and has antiplatelet effects as a Ca2+ antagonist with an IC50 of 155 μM.

1. Engeletin (Dihydrokaempferol 3-rhamnoside) may serve as a potential anti-inflammatory agent. 2. Engeletin possesses potent inhibition of PGE2 release with IC5 values of 19.6 μg ml. 3. Engeletin inhibits a recombinant human aldose reductase (IC5 value=1.16 microM).

Ranirestat (AS-3201) is an orally active and potent aldose reductase (AR) inhibitor with neuroprotective properties that ameliorates peripheral nerve dysfunction in rats with advanced diabetic polyneuropathy.Ranirestat inhibits the inflammatory response of high glucose-exposed endothelial cells and may be useful for the study of diabetic sensory-motor polyneuropathy.

beta-Glucogallin (beta-Glucogallin) is a selective aldose reductase (AKR1B1) inhibitor with antioxidant, anti-glycation, and anti-inflammatory properties. beta-Glucogallin is a naturally occurring compound derived from Emblica officinalis and is used in diabetes research. Vitamin B3-d4

Dutasteride (GI 198745) is a 5-alpha-reductase inhibitor that inhibits both type-1 and type2 isoforms of the enzyme and is used to treat benign prostatic hyperplasia.

2'-Acetylacteoside has antioxidative activity. It can significantly attenuate glutamate-induced neurotoxicity at concentrations ranging from 0.1 to 10 μM. 2'-Acetylacteoside shows antiproliferative effects on aortic smooth muscle, indicates that it may ha

AT-007 is an orally active CNS penetrant Aldose Reductase inhibitor for the treatment of Galactosemia (IC50: 100 pM). It reduces toxic galactitol levels and prevents disease complications in GALT deficiency rats.

DL-Glyceraldehyde (Glyceric aldehyde) is produced from the action of the enzyme glyceraldehyde dehydrogenase, which converts glycerol to glyceraldehyde using NADP as a cofactor. When present at sufficiently high levels, DL-Glyceraldehyde can be a cytotoxin and a mutagen. A cytotoxin is a compound that kills cells. A mutagen is a compound that causes mutations in DNA. DL-Glyceraldehyde is a highly reactive compound that can modify and cross-link proteins. DL-Glyceraldehyde modified proteins appear to be cytotoxic, depress intracellular glutathione levels, and induce reactive oxygen species (ROS) production (PMID: 14981296 ). DL-Glyceraldehyde has been shown to cause chromosome damage to human cells in culture and is mutagenic in the Ames bacterial test.

Epalrestat (ONO2235), an aldose reductase inhibitor, is well tolerated in Long-term therapy. It can effectually ameliorate the associated symptoms of diabetic neuropathy and delay the progression of the disease, particularly in patients with limited microangiopathy and good glycemic control.

Ponalrestat is an aldose reductase inhibitor.

D-Methionine sulfoxide inhibits peptide methionine sulfoxide reductase and can be used to inhibit ochre mites.D-Methionine sulfoxide can be added to chicken feed to promote growth.

Poliumoside is a natural compound which exhibits significant inhibition of advanced glycation end product formation with IC50 value of 4.6-25.7 μM, it also exhibits great inhibitory effects on rat lens aldose reductase with IC50 values of 0.85 μM.Poliumos

BYAKANGELICIN,a main furanocoumarin constituent isolated and characterized as an aldose reductase inhibitor,and is effective for the treatment of sugar cataracts and diabetic neuropathy and hence might be useful as a lead compound for the development of new type drugs for clinical use.

Alpha-Estradiol (Epiestradiol) is an estrogen that inhibits 5alpha-reductase and has potential in the study of androgenetic alopecia.

Tectoridin (Shekanin) possesses an estrogenic and thyroid hormone-like agent by activating estrogen and thyroid hormone receptors. Tectoridin has anti-oxidant, anti-inflammatory and hypoglycemic activities; Tectoridin and its five metabolites inhibits the activities of lens aldose reductase in rat (IC : 1.4-15.5 μM).

Finasteride (MK-906) is an oral inhibitor of active testosterone 5-alpha-reductase and Ki value is 10 nM.

Tolrestat (AY-27773) is a potent inhibitor of aldose reductase (IC50 = 35 nM).

Quercetin 3-gentiobioside (Quercetin-3-gentiobioside) is an inhibitor of AR and AGE formation and can be extracted from A. iwayomogi.Quercetin 3-gentiobioside inhibits the biological activity of aldose reductase (AR) and the formation of advanced glycosylation end products (AGEs).

Zopolrestat (CP 73850) is a potent inhibitor of aldose reductase (IC50 = 3.1 nM).

Gonadorelin Acetate (33515-09-2 free base) (Luteinizing Hormone Releasing Hormone (LH-RH)) is hypothalamic neuropeptide which plays a key role in the control of reproductive functions.

Lidorestat (IDD-676) is an aldose reductase inhibitor (IC50: 5 nM) with effective, selective and oral activity. Lidorestat improves nerve conduction and reduces the formation of cataracts. Lidorestat can be used to treat complications of chronic diabetes.

6-Methoxytricin, a flavonoid isolated from Centella asiatica, is an inhibitor of aldose reductase (AR) and advanced glycosylation end-products (AGE), and inhibits T-cell proliferation and activation in biologic cells.

Sulindac sulfone is a metabolite of the nonsteroidal anti-inflammatory drug sulindac.

Alrestatin (AY-22284) is a specific inhibitor of aldose reductase and attenuates glucose-induced angiotensin II production in rat vascular smooth muscle in vitro.

12-O-Methylcarnosic acid is a diterpene carnosic acid isolated from Salvia microphylla, is an active constituent of 5α-Reductase inhibition with an IC50 value of 61.7 μM. 12-O-Methylcarnosic acid has Antioxidant activity, it is effective preventing gastric lesions. 12-O-Methylcarnosic acid can suppress melanin production with downregulation of Tyrosinase expression in HMV-II melanoma cells. 12-O-Methylcarnosic acid may have anti-diabetic activity, it is able to significantly activate peroxisome proliferator-activated receptor (PPAR)γ.

Minalrestat(ARI-509) is an orally active and potent aldose reductase inhibitor for the study of impaired microvascular reactivity in diabetic patients.

Izonsteride (LY320236) is a selective and potent 5alpha reductase inhibitor with dual action on the type I and type II isoforms of the enzyme.Izonsteride is used in the treatment of oncology and genitourinary disorders, and may be used in the study of prostate cancer.

Turosteride is a small molecule steroidal 5α-reductase (5α-reductase) inhibitor.Turosteride has antitumor activity for the treatment of oncologic diseases and genitourinary disorders, and may be used in the study of prostate cancer.

2-Chloro-1-(4-fluorobenzyl)benzimidazole is an inhibitor of aldose reductase (ALR2).

Isomer-Turosteride (Isomer-Turosteride(Isomer-137099-09-3)) is a novel 5 alpha-reductase inhibitor.The antiprostatic effect of Isomer-Turosteride in adult rats is associated with the inhibition of the conversion of T to DHT.Isomer-Turosteride induces a decrease in prostate DHT independent of a secondary increase in T. Isomer-Turosteride has anticancer activity and inhibits the growth of tumor cells. Turosteride has anticancer activity and inhibits the growth of tumor cells. Translated with www.DeepL.com/Translator (free version)

Imirestat (HOE 843) is an aldose reductase inhibitor that can be used in diabetes research.

1. Isocurcumenol inhibits 5α-reductase which converts testosterone to dihydrotestosterone (DHT).

(R)-Viloxazine Hydrochloride is the R-isomer of Viloxazine, a selective norepinephrine reuptake inhibitor (NRI) used as an antidepressant.

EBPC is an inhibitor of aldose reductase.

WJ-39 is an orally active aldose reductase (AR) inhibitor that ameliorates renal lesions in diabetic nephropathy through activation of Nrf2 signaling, and may be used to ameliorate renal insufficiency and fibrosis.WJ-39 inhibits oxidative stress and inhibits the activation of the inflammatory vesicle of the oligomerization structural domain-like receptor family, pyrin structural domain 3 (NLRP3).

ALR2-IN-1 is a potent and selective ALR2 inhibitor with an IC50 value of 1.42 μM. ALR2-IN-1 possesses both antiglycemic and antioxidant activities and can be used to study the complications of diabetes.

Risarestat (CT-112) is a potent aldose reductase inhibitor and thyroid hormone receptor (TR) antagonist for the treatment of hypoglycemia.

Triptocalline A, a compound from Salacia chinensis, inhibits rat lens aldose reductase.

Danshenol A has strong aldose reductase (AR) inhibitory activity, has IC50 of 0.10 microM which is comparable to that of epalrestat in clinical use. Danshenol A also has antitumor activity in T-24, QGY, K562, Me180 and BIU87 cell lines, shows inhibited growth of K562 (IC50 = 0.53 μg/mL), T-24 (IC50 = 7.94 μg/mL), QGY (IC50 = 4.65 μg/mL) and Me180 (IC50 = 6.89 μg/mL) cell lines.

Fidarestat is an aldose reductase inhibitor (IC50s: 26 nM, 33 μM, and 1.8 μM for aldose reductase, AKR1B10, and V301L AKR1B10, respectively). It has the potential to treat diabetic disease.

8-Lavandulylkaempferol exhibits significant inhibitory effects with IC(50) values of 7.10 and 8.11 microM for butyrylcholinesterase and acetylcholinesterase, respectively. It shows inhibitory activities against aldose reductase, with the the IC50 of 0.79 microM.

Torilin is an inhibitor of testosterone 5 alpha-reductase, it (IC50 = 31.7 + - 4.23 microM) shows a stronger inhibition of 5 alpha-reductase than alpha-linolenic acid (IC50 = 160.3 + - 24.62 microM) but is weaker than finasteride (IC50 = 0.38 + - 0.06 microM). Torilin has immunomodulatory, hepatoprotective, and anti-inflammatory properties, it inhibits inflammation by limiting TAK1-mediated MAP kinase and NF-κB activation, it can attenuate arthritis severity, modify leukocyte activations in dLNs or joints, and restore serum and splenocyte cytokine imbalances. Torilin inhibits melanin production in alpha-melanocyte stimulating hormone-activated B16 melanoma cells, with an IC(50) value of 25 microM. Torilin shows excellent antimicrobial activity against Bacillus subtilis ATCC 6633 spores and vegetative cells. Torilin has a potent anti-angiogenic activity both in vivo and in vitro, and it may have a strong activity to suppress tumorigenesis by inhibition of tumor invasion, it reverses multidrug-resistance in cancer cells, it can potentiate the cytotoxicities of adriamycin, vinblastine, taxol and colchicine against multidrug-resistant KB-V1 and MCF7 ADR cells.