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Nepafenac(CAS#78281-72-8) Featured Image
  • Nepafenac(CAS#78281-72-8) 1

Nepafenac(CAS#78281-72-8)

Chemical Property:

Molecular Formula C15H14N2O2
Molar Mass 254.28
Density 1.249g/cm3
Melting Point 177-181°C
Boling Point 562.5°C at 760 mmHg
Flash Point 294°C
Water Solubility 0.014 mg/mL in water
Solubility DMSO 51 mg/mL Water <1 mg/mL Ethanol 4 mg/mL
Vapor Presure 1.11E-12mmHg at 25°C
Appearance powder
Color faint yellow to dark yellow
Merck 14,6469
Storage Condition room temp
Sensitive Sensitive to heat
Refractive Index 1.641
MDL MFCD08067732
In vivo study Nepafenac showed significantly greater ocular bioavailability, and amfenac had greater COX-2 inhibitory activity than either ketorolac or bromfenac. Nepafenac showed weak COX-1 inhibitory activity with an IC50 of 64.3 mM. In rabbits, Nepafenac inhibited prostaglandin synthesis in the IRIS/ciliary body (85-95%) and retina/choroid (55%). Nepafenac(0.5%) resulted in a 65% reduction in retinal edema, which was associated with a 62% inhibition of blood-retinal barrier breakdown. Nepafenac(0.5%) significantly inhibited (46%) blood-retinal barrier disruption, accompanied by almost complete inhibition of PGE2 synthesis (96%). Nepafenac significantly inhibits retinal prostaglandin E(2), superoxide, cyclooxygenase-2, and leukostasis in the retinal microvasculature of insulin-deficient diabetic rats, does not affect vascular endothelial growth factor (VEGF) and nitric oxide (NO). In diabetic rats, Nepafenac significantly inhibited the number of transferase-mediated dUTP Nick end-labeled positive capillary cells, acellular capillaries, and pericytes. In mice, Nepafenac resulted in significantly reduced choroidal neovascularization and ischemia-Induced Retinal neovascularization compared to controls. Nepafenac also attenuated ischemia-induced increases in retinal VEGF mRNA expression. In ocular and metastatic animal models, Nepafenac delays the progression of malignancy, as well as the reduction in the weight of uveal melanoma.

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Product Tags

Hazard Symbols N – Dangerous for the environment
Risk Codes 50/53 – Very toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment.
Safety Description S60 – This material and its container must be disposed of as hazardous waste.
S61 – Avoid release to the environment. Refer to special instructions / safety data sheets.
UN IDs UN 3077 9 / PGIII
WGK Germany 3
RTECS CY1480710

 

 

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