Epalrestat - CAS 82159-09-9
Catalog number:
82159-09-9
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C15H13NO3S2
Molecular Weight:
319.4
COA:
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Targets:
Aldose Reductase
Description:
Epalrestat is an aldose reductase inhibitor with IC50 of 72 nM.
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Purity:
>98%
MSDS:
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1.Epalrestat protects against diabetic peripheral neuropathy by alleviating oxidative stress and inhibiting polyol pathway.
Li QR1, Wang Z1, Zhou W2, Fan SR1, Ma R1, Xue L1, Yang L1, Li YS2, Tan HL2, Shao QH2, Yang HY1. Neural Regen Res. 2016 Feb;11(2):345-51. doi: 10.4103/1673-5374.177745.
Epalrestat is a noncompetitive and reversible aldose reductase inhibitor used for the treatment of diabetic neuropathy. This study assumed that epalrestat had a protective effect on diabetic peripheral nerve injury by suppressing the expression of aldose reductase in peripheral nerves of diabetes mellitus rats. The high-fat and high-carbohydrate model rats were established by intraperitoneal injection of streptozotocin. Peripheral neuropathy occurred in these rats after sustaining high blood glucose for 8 weeks. At 12 weeks after streptozotocin injection, rats were intragastrically administered epalrestat 100 mg/kg daily for 6 weeks. Transmission electron microscope revealed that the injuries to myelinated nerve fibers, non-myelinated nerve fibers and Schwann cells of rat sciatic nerves had reduced compared to rats without epalrestat administuation. Western blot assay and immunohistochemical results demonstrated that after intervention with epalrestat, the activities of antioxidant enzymes such as superoxide dismutase, catalase and glutathione peroxidase gradually increased, but aldose reductase protein expression gradually diminished.
2.Hyperglycemia Promotes Schwann Cell De-differentiation and De-myelination via Sorbitol Accumulation and Igf1 Protein Down-regulation.
Hao W1, Tashiro S2, Hasegawa T3, Sato Y4, Kobayashi T5, Tando T1, Katsuyama E1, Fujie A1, Watanabe R1, Morita M6, Miyamoto K1, Morioka H1, Nakamura M1, Matsumoto M1, Amizuka N3, Toyama Y1, Miyamoto T7. J Biol Chem. 2015 Jul 10;290(28):17106-15. doi: 10.1074/jbc.M114.631291. Epub 2015 May 21.
Diabetes mellitus (DM) is frequently accompanied by complications, such as peripheral nerve neuropathy. Schwann cells play a pivotal role in regulating peripheral nerve function and conduction velocity; however, changes in Schwann cell differentiation status in DM are not fully understood. Here, we report that Schwann cells de-differentiate into immature cells under hyperglycemic conditions as a result of sorbitol accumulation and decreased Igf1 expression in those cells. We found that de-differentiated Schwann cells could be re-differentiated in vitro into mature cells by treatment with an aldose reductase inhibitor, to reduce sorbitol levels, or with vitamin D3, to elevate Igf1 expression. In vivo DM models exhibited significantly reduced nerve function and conduction, Schwann cell de-differentiation, peripheral nerve de-myelination, and all conditions were significantly rescued by aldose reductase inhibitor or vitamin D3 administration.
3.Aldo-keto reductase 1B10 protects human colon cells from DNA damage induced by electrophilic carbonyl compounds.
Zu X1,2, Yan R2, Pan J3, Zhong L2, Cao Y2, Ma J2, Cai C4, Huang D4, Liu J1, Chung FL3, Liao DF4, Cao D2,4. Mol Carcinog. 2016 Mar 10. doi: 10.1002/mc.22477. [Epub ahead of print]
Electrophilic carbonyl compounds are highly cytotoxic and genotoxic. Aldo-keto reductase 1B10 (AKR1B10) is an enzyme catalyzing reduction of carbonyl compounds to less toxic alcoholic forms. This study presents novel evidence that AKR1B10 protects colon cells from DNA damage induced by electrophilic carbonyl compounds. AKR1B10 is specifically expressed in epithelial cells of the human colon, but this study found that AKR1B10 expression was lost or markedly diminished in colorectal cancer, precancerous tissues, and a notable portion of normal adjacent tissues (NAT). SiRNA-mediated silencing of AKR1B10 in colon cancer cells HCT-8 enhanced cytotoxicity of acrolein and HNE, whereas ectopic expression of AKR1B10 in colon cancer cells RKO prevented the host cells against carbonyl cytotoxicity. Furthermore, siRNA-mediated AKR1B10 silencing led to DNA breaks and activation of γ-H2AX protein, a marker of DNA double strand breaks, particularly in the exposure of HNE (10 μM).
4.Color polymorphs of aldose reductase inhibitor epalrestat: configurational, conformational and synthon differences.
Swapna B1, Suresh K1, Nangia A1. Chem Commun (Camb). 2016 Mar 3;52(21):4037-40. doi: 10.1039/c6cc00697c.
We report five crystalline polymorphs and an amorphous phase of epalrestat together with configurational isomerism and color behavior: form I (deep red), form II (deep orange), form III (bright yellow), form IV (yellow), and form V (orange) are in the E,Z configuration of the drug, and a Z,Z isomer (bright yellow). Two pathways are identified for polymorph conversion: direct transformation of the E,Z isomer and another pathway via the Z,Z isomer to the E,Z polymorphs. From a pharmaceutical perspective, the stability of polymorphs was established under grinding, solvent slurry and thermal conditions: form I (thermodynamic) > form II > form V > form III > form IV (least stable).
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CAS 82159-09-9 Epalrestat

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