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Merck
CN

SML0527

Epalrestat

≥98% (HPLC)

别名:

(5Z)-5-[(2E)-2-Methyl-3-phenyl-2-propen-1-ylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid

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关于此项目

经验公式(希尔记法):
C15H13NO3S2
化学文摘社编号:
分子量:
319.40
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
protect from light
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Quality Level

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

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

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

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.

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


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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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
Mary Ann Ramirez et al.
Pharmacotherapy, 28(5), 646-655 (2008-05-02)
Diabetic neuropathy is one of the most common long-term complications in patients with diabetes mellitus, with a prevalence of 60-70% in the United States. Treatment options include antidepressants, anticonvulsants, tramadol, and capsaicin. These agents are modestly effective for symptomatic relief
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
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
Zaniar Ghazizadeh et al.
iScience, 25(4), 104153-104153 (2022-04-19)
The sinoatrial node (SAN) is the primary pacemaker of the heart. The human SAN is poorly understood due to limited primary tissue access and limitations in robust in vitro derivation methods. We developed a dual SHOX2:GFP; MYH6:mCherry knockin human embryonic stem

全球贸易项目编号

货号GTIN
SML0527-50MG04061832723563
SML0527-10MG04061837084768

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