CP 73850

Modify Date: 2024-01-06 16:12:04

CP 73850 Structure
CP 73850 structure
Common Name CP 73850
CAS Number 110703-94-1 Molecular Weight 419.37700
Density 1.58g/cm3 Boiling Point 598.7ºC at 760mmHg
Molecular Formula C19H12F3N3O3S Melting Point N/A
MSDS Chinese USA Flash Point 315.9ºC
Symbol GHS06
GHS06
Signal Word Danger

 Use of CP 73850


Zopolrestat (CP73850) is a potent, orally active aldose reductase (AR) inhibitor with an IC50 of 3.1 nM. Zopolrestat is used for the research of diabetic complications[1].

 Names

Name Zopolrestat
Synonym More Synonyms

 CP 73850 Biological Activity

Description Zopolrestat (CP73850) is a potent, orally active aldose reductase (AR) inhibitor with an IC50 of 3.1 nM. Zopolrestat is used for the research of diabetic complications[1].
Related Catalog
In Vitro Zopolrestat is a potent inhibitor of the reduction of both glyceraldehyde and glucose by the human and rat enzymes[1].
In Vivo Zopolrestat (2.5 mg/kg-50 mg/kg; p.o.; once-a-day for 5 days) and left untreated for 7 days) prevents accumulation of sorbitol in the kidney cortex of diabetic rats and normalize elevated renal blood flow in galactosemic rats[1]. Animal Model: Male Sprague-Dawley rats (made diabetic by iv injection of streptozotocin)[1]. Dosage: 2.5 mg/kg-50 mg/kg Administration: P.o.; once-a-day for 5 days Result: Its ED50s in reversing already elevated sorbitol accumulation in rat sciatic nerve, retina, and lens in a chronic test were 1.9, 17.6, and 18.4 mg/kg, respectively.
References

[1]. Mylari BL, et al. Novel, potent aldose reductase inhibitors: 3,4-dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl] methyl]-1-phthalazineacetic acid (zopolrestat) and congeners. J Med Chem. 1991;34(1):108-122.

 Chemical & Physical Properties

Density 1.58g/cm3
Boiling Point 598.7ºC at 760mmHg
Molecular Formula C19H12F3N3O3S
Molecular Weight 419.37700
Flash Point 315.9ºC
Exact Mass 419.05500
PSA 113.32000
LogP 3.70040
Vapour Pressure 3.5E-15mmHg at 25°C
Index of Refraction 1.683

 Safety Information

Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H301-H413
Precautionary Statements P301 + P310
Hazard Codes T+
RIDADR UN 2811 6.1 / PGIII

 Articles24

More Articles
Inhibiting wild-type and C299S mutant AKR1B10; a homologue of aldose reductase upregulated in cancers.

Eur. J. Pharmacol. 584 , 213-221, (2008)

AKR1B10 is an aldose reductase (AR) homologue overexpressed in liver cancer and various forms of that enzyme in carcinomas catalyze the reduction of anticancer drugs, potential cytostatic drug, and dl...

Mediation of aldose reductase in lipopolysaccharide-induced inflammatory signals in mouse peritoneal macrophages.

Cytokine 36(3-4) , 115-22, (2006)

Aldose reductase (AR; AKR1B1) a member of aldo-keto reductase super family, that we had shown earlier mediates cytotoxic signals induced by high glucose, cytokines and growth factors, also mediates th...

Endotoxin causes pulmonary hypertension by upregulating smooth muscle endothelin type-B receptors: role of aldose reductase.

Shock 30(2) , 189-96, (2008)

Endothelin-1 (ET-1), a potent vasoconstrictor and mitogen, is upregulated in pulmonary tissue during endotoxemia and contributes markedly to endotoxin-induced pulmonary hypertension. It is, however, u...

 Synonyms

2-[4-oxo-3-[[5-(trifluoromethyl)-1,3-benzothiazol-2-yl]methyl]phthalazin-1-yl]acetic acid
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