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Epalrestat

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Epalrestat Basic information

Product Name:
Epalrestat
Synonyms:
  • 3-thiazolidineaceticacid,5-(2-methyl-3-phenyl-2-propenylidene)-4-oxo-2-thioxo
  • 5-((1z,2e)-2-methyl-3-phenylpropenylidene)-4-oxo-2-thioxo-3-thiazolidineacet
  • e)-(e
  • EPALRESTAT
  • (e,e)-2-[5-(2-methyl-3-phenyl-prop-2-enylidene)-4-oxo-2-sulfanylidene-thiazo lidin-3-yl]acetic acid
  • AKOS BBS-00007767
  • OTAVA-BB BB7211260020
  • Epalrest
CAS:
82159-09-9
MF:
C15H13NO3S2
MW:
319.4
EINECS:
675-018-0
Product Categories:
  • API
  • Hormone Drugs
  • Aromatics
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Treatment of diabetic neuropathy
  • API's
  • Sulfur & Selenium Compounds
  • 82159-09-9
Mol File:
82159-09-9.mol
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Epalrestat Chemical Properties

Melting point:
210-217 C
Boiling point:
516.8±60.0 °C(Predicted)
Density 
1.43±0.1 g/cm3(Predicted)
storage temp. 
-20°C
solubility 
DMSO: soluble5mg/mL, clear (warmed)
pka
3.62±0.10(Predicted)
form 
powder
color 
yellow to orange
Merck 
14,3605
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
InChI
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-
InChIKey
CHNUOJQWGUIOLD-NFZZJPOKSA-N
SMILES
S1/C(=C\C(\C)=C\C2=CC=CC=C2)/C(=O)N(CC(O)=O)C1=S
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Safety Information

RIDADR 
2811
WGK Germany 
3
RTECS 
XJ5131855
HS Code 
2932.99.7000
HazardClass 
6.1
PackingGroup 
II

MSDS

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Epalrestat Usage And Synthesis

Description

Epalrestat is the second aldose reductase inhibitor to be introduced worldwide and the first to be launched in Japan. The compound is indicated for the treatment of diabetic neuropathy. It is also being investigated for diabetic retinopathy and nephropathy.

Chemical Properties

Red Solid

Originator

Ono (Japan)

Uses

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

Uses

Epalrestat is an aldose reductase inhibitor with IC50 of 72 nM

Uses

An aldose reductase inhibitor. It is used in treatment of diabetic neuropathy.

Definition

ChEBI: A monocarboxylic acid that is 1,3-thiazolidine which is substituted on the nitrogen by a carboxymethyl group, at positions 2 and 4 by thioxo and oxo groups, respectively, and at position 5 by a 2-methyl-3-phenylprop-2-en-1-ylidene group. It is an inhibitor of aldose reductase (which catalyses the conversion of glucose to sorbitol) and is used for the treatment of some diabetic complications, including neuropathy.

brand name

Kinedak

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.

References

1) Kikkawa?et al. (1983)?Effect of a new aldose reductase inhibitor, (E)-3-carboxymethyl-5-[(2E)-methyl-3-phenylpropenylidene]rhodanine (ONO-2235), on peripheral nerve disorders in streptozotocin diabetic rats; Diabetologica,?24?290 2) Terashima?et al. (1984)?Effects of a new aldose reductase inhibitor on various tissues in vitro; J. Pharmacol. Exp. Ther.,?229?226 3) Ramirez and Borja (2008)?Epalrestat: an aldose reductase inhibitor for the treatment of diabetic neuropathy; Pharmacotherapy,?28?646

EpalrestatSupplier

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