SML0527
Epalrestat
≥98% (HPLC)
别名:
(5Z)-5-[(2E)-2-Methyl-3-phenyl-2-propen-1-ylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid
产品名称
Epalrestat, ≥98% (HPLC)
SMILES string
S1\C(=C/C(=C/c2ccccc2)/C)\C(=O)N(C1=S)CC(=O)O
InChI
1S/C15H13NO3S2/c1-10(7-11-5-3-2-4-6-11)8-12-14(19)16(9-13(17)18)15(20)21-12/h2-8H,9H2,1H3,(H,17,18)/b10-7+,12-8-
InChI key
CHNUOJQWGUIOLD-NFZZJPOKSA-N
assay
≥98% (HPLC)
form
powder
storage condition
protect from light
color
yellow to orange
solubility
DMSO: 5 mg/mL, clear (warmed)
storage temp.
−20°C
Quality Level
Biochem/physiol Actions
Epalrestat inhibits Aldose Reductase (AR) involved in the rate limiting step in the conversion of glucose to sorbitol under hyperglycemic conditions. Aldose reductase has been the target of multiple clinical investigatons to treat diabetic neuropathy and retinopathy. Epalrestat is an approved drug in Japan and India, used for the treatment of diabetic neuropathy.
Epalrestat is an Aldose Reductase inhibitor.
Application
Epalrestat has been used as an aldose reductase inhibitor:
- in the dahomey larvae diet fed forDrosophila
- for non-irradiated and X-ray irradiated human aldose reductase
- to test its protective effect in mice with bleomycin-induced pulmonary fibrosis
Features and Benefits
This compound is featured on the Dopamine and Norepinephrine Metabolism page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Other Notes
Light sensitve
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Hyun Ah Jung et al.
The Journal of pharmacy and pharmacology, 60(9), 1227-1236 (2008-08-23)
Important targets for the prevention and treatment of diabetic complications include aldose reductase (AR) inhibitors (ARIs) and inhibitors of advanced glycation endproduct (AGE) formation. Here we evaluate the inhibitory activities of prenylated flavonoids isolated from Sophora flavescens, a traditional herbal
Zhen-Yu Li et al.
The American journal of Chinese medicine, 41(4), 801-815 (2013-07-31)
The lignan extracts from the tree bark of Eucommia ulmoides Oliv., a famous traditional Chinese medicine, have been demonstrated to have inhibitory effects on aldose reductase activity in spontaneously hypertensive rat myocardium. This study was aimed to investigate the hypertensive
Juan Gu et al.
Journal of ethnopharmacology, 133(1), 6-13 (2010-09-08)
To investigate the effects of lignans extracted from Eucommia ulmoides and epalrestat on vascular remodeling in spontaneously hypertensive rats. Ten-week-old male spontaneously hypertensive rats were randomly divided into 3 groups (12 rats each group), and treated orally with 100 mg/kg/d
Bruno Bulic et al.
Neuropharmacology, 59(4-5), 276-289 (2010-02-13)
Alzheimer disease is characterized by pathological aggregation of two proteins, tau and Abeta-amyloid, both of which are considered to be toxic to neurons. In this review we summarize recent advances on small molecule inhibitors of protein aggregation with emphasis on
J W Steele et al.
Drugs & aging, 3(6), 532-555 (1993-11-01)
Epalrestat is a carboxylic acid derivative which inhibits aldose reductase, an enzyme of the sorbitol (polyol) pathway. Under hyperglycaemic conditions epalrestat reduces intracellular sorbitol accumulation, which has been implicated in the pathogenesis of late-onset complications of diabetes mellitus. Epalrestat 150
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