Epalrestat
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
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
MSDS
- Language:English Provider:Epalrestat
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
Epalrestat Preparation Products And Raw materials
Raw materials
EpalrestatSupplier
- Tel
- 17080805366
- 17080805366@126.com
- Tel
- 0371-65741762
- sales@hasunny.com
- Tel
- +86-21-52210535 +86-13162045318
- sales@jinhchem.com
- Tel
- 025-85760569 13814067126
- litianang@caremo.com.cn
- Tel
- 13576915071
- taisinor@vip.163.com
Epalrestat(82159-09-9)Related Product Information
- 2,2'-Dithiobis(benzothiazole)
- Triphenyltin acetate
- PHENYL VALERATE
- Fosthiazate
- Acetonitrile
- Methylparaben
- Methyl acrylate
- Methyl acetate
- Kresoxim-methyl
- Methylchloroisothiazolinone/methylisothiazolinone mixture (MCIT/MIT)
- Paraquat dichloride
- Basic Violet 1
- Benzothiazole
- Methanol
- 1-Phenyl-2-nitropropene
- 4-oxo-2-mercapto-thiazole-3-acetic acid (intermediate of epalrestat)
- Brexpiprazole
- 4-oxo-5-[(2E)-3-phenyl-2-propen-1-ylidene]-2-thioxo-, (5Z)-