Zopolrestat - CAS 110703-94-1
Catalog number: B0084-358923
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C19H12F3N3O3S
Molecular Weight:
419.38
COA:
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Targets:
Aldose Reductase
Description:
Zopolrestat is an inhibitor of Aldose Reductase(AR). It has been shown to play roles in inflammation and cancer. It is used for the treatment of diabetic nephropathy and cardiac disease. It was developed by Pfizer and was terminated in clinic phase 2 trials.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-358923 25 mg $198 In stock
B0084-358923 50 mg $298 In stock
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Purity:
95%
Appearance:
Off white to light brown powder
Synonyms:
3-[(5-Trifluoromethyl-2-benzothiazolyl)methyl]-3,4-dihydro-4-oxophthalazine-1-acetic acid;CP-73850;3,4-Dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl]methyl]-1-phthalazineacetic acid;Alond;Xedia;2-[4-Oxo-3-[[5-(trifluoromethyl)-1,3-benzothiazol-2-yl]methyl]phthalazin-1-yl]acetic acid;CP 73850; CP73850; CP-73850; Zopolrestat; Zopolrestatum
Solubility:
DMSO: ≥20 mg/mL
Storage:
2-8ºC
MSDS:
Inquire
Application:
Zopolrestat is used for the treatment of diabetic nephropathy and cardiac disease.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Grams to Kilograms
Boiling Point:
598.7±60.0 °C | Condition: Press: 760 Torr
Melting Point:
197-198 °C
Density:
1.58±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
BCSVCWVQNOXFGL-UHFFFAOYSA-N
InChI:
InChI=1S/C19H12F3N3O3S/c20-19(21,22)10-5-6-15-14(7-10)23-16(29-15)9-25-18(28)12-4-2-1-3-11(12)13(24-25)8-17(26)27/h1-7H,8-9H2,(H,26,27)
Canonical SMILES:
C1=CC=C2C(=C1)C(=NN(C2=O)CC3=NC4=C(S3)C=CC(=C4)C(F)(F)F)CC(=O)O
Current Developer:
Zopolrestat was developed by Pfizer and was terminated in clinic phase 2 trials.
1.Aldose reductase inhibitors zopolrestat and ferulic acid alleviate hypertension associated with diabetes: effect on vascular reactivity.
Badawy D1, El-Bassossy HM, Fahmy A, Azhar A. Can J Physiol Pharmacol. 2013 Feb;91(2):101-7. doi: 10.1139/cjpp-2012-0232. Epub 2013 Feb 11.
This study investigated the effect of aldose reductase (AR) inhibitors on hypertension in diabetes. Diabetes was induced with streptozotocin, while AR inhibitors zopolrestat and ferulic acid were administered at 2 weeks after streptozotocin treatment and for 6 weeks afterwards. Then, blood pressure (BP) and serum level of glucose were determined. Concentration-response curves for phenylephrine (PE), KCl, and acetylcholine (ACh) were obtained in isolated aorta. In addition, ACh-induced NO and reactive oxygen species (ROS) generation in aorta and histopathology were examined. Compared with the control animals, diabetes increased diastolic and systolic BP. AR inhibitors reduced diastolic BP elevation without affecting the developed hyperglycaemia. Diabetes increased the contractile response of aorta to KCl, and decreased the relaxation response to Ach, while administering AR inhibitors prevented an impaired response to ACh. Incubation of aorta isolated from diabetic animals with AR inhibitors did not affect the impaired relaxation response to ACh.
2.Zopolrestat Induced Suicidal Death of Human Erythrocytes.
Bouguerra G, Bissinger R, Abbès S, Lang F. Cell Physiol Biochem. 2015;37(4):1537-46. doi: 10.1159/000438521. Epub 2015 Oct 30.
BACKGROUND/AIMS: The aldose reductase inhibitor zopolrestat has been shown to either decrease or increase apoptosis, the suicidal death of nucleated cells. Erythrocytes may similarly enter suicidal death or eryptosis, which is characterized by cell shrinkage and cell membrane scrambling with phosphatidylserine translocation to the erythrocyte surface. Triggers of eryptosis include oxidative stress, Ca2+ entry with increase of cytosolic Ca2+ activity ([Ca2+]i), and ceramide formation. The present study explored, whether and how zopolrestat induces eryptosis.
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