Epalrestat

Bezeichnung:Epalrestat

CAS-Nr82159-09-9

Englisch Name:Epalrestat

CBNumberCB6312501

SummenformelC15H13NO3S2

Molgewicht319.4

MOL-Datei82159-09-9.mol

Epalrestat physikalisch-chemischer Eigenschaften

Schmelzpunkt	210-217 C
Siedepunkt	516.8±60.0 °C(Predicted)
Dichte	1.43±0.1 g/cm3(Predicted)
storage temp.	-20°C
Löslichkeit	DMSO: soluble5mg/mL, clear (warmed)
pka	3.62±0.10(Predicted)
Aggregatzustand	powder
Farbe	yellow to orange
Merck	14,3605
Stabilität	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

Sicherheit

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

Gefahreninformationscode (GHS)

Epalrestat Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Chemische Eigenschaften
Red Solid
Originator
Ono (Japan)
Verwenden
An aldose reductase inhibitor. It is used in treatment of diabetic neuropathy.
Verwenden
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
Verwenden
Epalrestat is an aldose reductase inhibitor with IC50 of 72 nM
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.
Trademarks
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.
Einzelnachweise
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 Upstream-Materialien And Downstream Produkte

Epalrestat Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

82159-09-9, Epalrestat Verwandte Suche:

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