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Merck

SML0527

Epalrestat

≥98% (HPLC)

別名:

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

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この商品について

実験式(ヒル表記法):
C15H13NO3S2
CAS番号:
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

関連するカテゴリー

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

保管分類

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

SML0527-50MG: + SML0527-10MG: + SML0527-VAR: + SML0527-BULK:

jan


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試験成績書(COA)

Lot/Batch Number

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以前この製品を購入いただいたことがある場合

文書ライブラリで、最近購入した製品の文書を検索できます。

文書ライブラリにアクセスする

Vincenzo Calderone et al.
The Journal of pharmacy and pharmacology, 62(1), 107-113 (2010-08-21)
Many observations report the cardioprotective effects of inhibitors of aldose reductase in different models of ischaemia-reperfusion injury in diabetic myocardium. In this paper, the inhibitory effects of the new pyrido[1,2-a]-pyrimidin-4-one derivative PPO, whose aldose reductase-inhibitory and antioxidant effects were shown
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
Ramakrishna Nirogi et al.
Journal of pharmaceutical and biomedical analysis, 74, 227-234 (2012-12-19)
A simple and rapid LC-MS/MS method was developed and validated for the quantification of epalrestat, an aldose reductase inhibitor for the treatment of diabetic neuropathy. Following protein precipitation epalrestat and IS were eluted with 10mM ammonium acetate and acetonitrile using
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
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

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