Aldose Reductase Inhibitor

AKR1B1/STAT3/SLC7A11-regulator-1 (5a) is an AKR1B1/STAT3/SLC7A11 regulator that reverses DOX resistance in MCF-7/ADR cells by enhancing ferroptosis activity. AKR1B1/STAT3/SLC7A11-regulator-1 can be used in breast cancer research.

Asperaldin is a potent aldose reductase (RLAR) inhibitor found in Aspergillus niger CFR-1046.

Adhumulone is an α-acid derived from hops and a selective AKR1B10 inhibitor, with IC₅₀ values of 5.41-29.27 μM and K_i values of 3.27-16.79 μM against human AKR1B10. Adhumulone inhibits AKR1B10-mediated reduction of Farnesol (HY-Y0248A) as a competitive inhibitor, and it also suppresses the reduction of DL-Glyceraldehyde (HY-128748) and Farnesal substrates. Adhumulone is useful for research on ras-dependent malignancies.

ALR2-IN-8 is a potent aldose reductase (ALR2/AKR1B1) inhibitor with a K_I of 7.34 nM. ALR2-IN-8 has extremely low toxicity to normal cells and has a weak direct killing effect on cancer cells. ALR2-IN-8 can used for the studies of diabetic and inflammation-linked disorders.

PTP1B/AKR1B1-IN-1 is a dual inhibitor of protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), with IC₅₀s of 0.06 μM and 4.3 μM, respectively. PTP1B/AKR1B1-IN-1 also inhibits TC-PTP with an IC₅₀ value of 9 μM. PTP1B/AKR1B1-IN-1 serves as an insulin-mimetic agent in murine myoblasts, and reduces AKR1B1-dependent sorbitol accumulation. PTP1B/AKR1B1-IN-1 inhibits development of type 2 diabetes mellitus (T2DM) to control blood glucose levels.

IDD388 is a selective aldose reductase (ALR2) inhibitor with an IC₅₀ of 30 nM. IDD388 displays selectivity for ALR2 over ALR1 (IC₅₀ of 14 μM).

ALR2-IN-2 is a potent inhibitor of aldose reductase (ALR2), with IC₅₀s of 22 nM and 116 nM for rat ALR2 and ALR1, respectively. ALR2-IN-2 can be used for the research of diabetic complications.

APPA is an aldose reductase inhibitor. APPA can effectively prevent apoptosis and the symptoms of Streptozotocin (HY-13753)-induced diabetes by inhibiting the polyol pathway in rats. APPA has the potential for diabetic nephropathy (DN) research.

Minalrestat (ARI-509) is a potent and orally active aldose reductase inhibitor. Minalrestat can be used in the research of diabetes.

PTP1B/AKR1B1-IN-2 (Compound 7f) is a dual PTP1B/AKR1B1 inhibitor (IC₅₀s: 3.2 and 2.1 μM, K_is: 4.0 and 0.9μM). PTP1B/AKR1B1-IN-2 is an insulin-mimetic agent. PTP1B/AKR1B1-IN-2 improves glucose uptake in murine C2C12 myoblasts. PTP1B/AKR1B1-IN-2 can be used for research of Type 2 diabetes mellitus (T2DM).

ALR1/2-IN-1 (Compound 6e) is an aldehyde reductase (ALR1) and aldose reductase (ALR2) inhibitor with IC₅₀ values of 3.26 μM and 3.06 μM against ALR1 and ALR2, respectively. ALR1/2-IN-1 shows anticancer activity.

Methosorbinil is an aldose reductase inhibitor with anti-cataract activity.

Myrciacetin is a flavonoid from Rhododendron dauricum. Myrciacetin is against rat lens aldose reductase with an IC₅₀ of 13 μM.

Dehydroglyasperin D inhibits rat and human Aldose Reductase (AR) (IC₅₀: 62.4 μM and 176.2 μM respectively). Dehydroglyasperin D has anti-obesity, antioxidant effects. Dehydroglyasperin D shows anti-inflammatory activity by inhibiting COX-2 expression and the MLK3 signaling pathway. Dehydroglyasperin D also inhibits melanin synthesis. Dehydroglyasperin D is a prenylated flavonoid that can be isolated from Glycyrrhiza uralensi.

ALR2-IN-7 (Compound 5a) is a highly potent and selective aldose reductase (ALR2/AKR1B1) inhibitor (K_i=8.71 nM). ALR2-IN-7 is promising for research of diabetic complications (e.g., retinopathy, nephropathy) and cancers.

Aldose reductase-IN-4 (compund IIc) is an aldose reductase inhibitor with IC₅₀s of 11.70 μM and 0.98 μM for aldehyde reductase 1 (ALR1) and ALR2, respectively.

Cemtirestat (CMTI) is a carboxymethylated thiatriazinoindole inhibitor of aldose reductase (ALR2). Cemtirestat potently inhibits rat ocular lens ALR2 with an IC₅₀ of 0.116 μM, and exhibits a 302-fold selectivity for rat kidney ALR1. Cemtirestat is applicable to the research of advanced diabetic complications.

(Rac)-Ganoderic acid C2 is the racemate of Ganoderic acid C2 (HY-N1517). Ganoderic acid C2 is a bioactive triterpenoid in Ganoderma lucidum. Ganoderic acid C2 possesses anti-tumor, antihistamine, anti-aging and cytotoxic effects. Ganoderic acid C2 exhibits high inhibitory activity against the rat lens aldose reductase (RLAR) with an IC50 of 3.8 µM[.

Esmolol hydrochloride solution is mainly composed of Esmolol hydrochloride (HY-B1392). Esmolol hydrochloride is an ultra-short-acting cardioselective β1-adrenergic blocker. Esmolol hydrochloride exerts its antiarrhythmic effect by activating Neurokinin 1 Receptor. Esmolol hydrochloride attenuates post resuscitation myocardial dysfunction. Esmolol hydrochloride improves diabetic wound healing by inhibiting aldose reductase and the production of advanced glycation end products and promoting fibroblast migration. Esmolol hydrochloride can be used to study cardiac diseases such as arrhythmias and diabetic foot ulcers.

Emodin-8-glucoside (Standard) is the analytical standard of Emodin-8-glucoside. This product is intended for research and analytical applications. Emodin-8-glucoside is an anthraquinone derivative that can be isolated from Aloe vera. Emodin-8-glucoside is the inhibitor for MAPK with an inhibition constant of 430.14 pM. Emodin-8-glucoside exhibits moderate inhibitory activity against rat lens aldose reductase (ALAR) and topoisomerases II with IC₅₀s of 14.4 μM and 66 μM. Emodin-8-glucoside exhibits antioxidant, anti-inflammatory and anti-fibrotic activities. Emodin-8-glucoside can cross the blood brain barrier.