[CAS NO. 78281-72-8] Nepafenac
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PRODUCTS SPECIFICATIONS [78281-72-8]
Distributor
Catalog
HY-17357
Brand
MCE
CAS
78281-72-8
DESCRIPTION [78281-72-8]
Overview
| MDL | MFCD08067732 |
|---|---|
| Molecular Weight | 254.28 |
| Molecular Formula | C15H14N2O2 |
| SMILES | O=C(N)CC1=CC=CC(C(C2=CC=CC=C2)=O)=C1N |
For research use only. We do not sell to patients.
Summary
Nepafenac(AHR 9434; AL 6515; Nevanac) is a selective COX-2 inhibitor ; is prodrug of Amfenac. IC50 value: Target: COX-2 Nepafenac is a NSAID (nonsteroidal anti inflammatory drug) that is routinely used in opthamology to control pain following cataract surgery.
IC50 & Target
|
COX-1 64.3 μM (IC 50 ) |
COX-2
|
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00332774 | Alcon Research |
Cataract
|
February 2006 | Phase 3 |
| NCT00348582 | Innovative Medical |
Cataract
|
Phase 4 | |
| NCT01318499 | Alcon Research |
Cataract
|
March 2011 | Phase 2 |
| NCT01853072 | Alcon Research |
Non-Proliferative Diabetic Retinopathy|Cataract
|
June 2013 | Phase 3 |
| NCT00900887 | Hospital Juarez de Mexico |
Diabetic Retinopathy|Macular Edema
|
April 2008 | Phase 2 |
| NCT01238783 | Alcon Research |
Bacterial Conjunctivitis
|
January 2011 | Phase 2 |
| NCT00333255 | Alcon Research |
Cataract
|
September 2005 | Phase 3 |
| NCT03406689 | University Hospital of Patras |
Pain
|
September 1, 2017 | Not Applicable |
| NCT00782717 | Alcon Research |
Macular Edema
|
November 2008 | Phase 2 |
| NCT04843839 | L.V. Prasad Eye Institute|Allergan |
Congenital Hereditary Endothelial Dystrophy of Cornea
|
December 15, 2020 | Phase 2 |
| NCT00347204 | Center For Excellence In Eye Care|Allergan |
Myopia|Hyperopia
|
January 2006 | Phase 4 |
| NCT02955641 | Sheba Medical Center |
Glaucoma, Closed-Angle|Glaucoma, Narrow-Angle|Glaucoma, Angle-Closure
|
November 1, 2016 | Not Applicable |
| NCT05072262 | Oslo University Hospital |
Descemet Stripping Automated Endothelial Keratoplasty (DSAEK)|Descemet Membrane Endothelial Keratoplasty (DMEK)
|
May 2022 | Phase 4 |
| NCT00377546 | Innovative Medical |
Vitrectomy
|
Phase 4 | |
| NCT03851172 | Assiut University |
Cataract|Miosis
|
March 1, 2019 | Phase 2 |
| NCT02084576 | Hospital Oftalmologico de Brasilia |
Cystoid Macular Edema|Cataract
|
August 2013 | Phase 4 |
| NCT00865540 | Clinica Oftamologica Zona Sul |
Cataract
|
March 2009 | Phase 4 |
| NCT02752646 | MDbackline, LLC|Alcon Research |
Cataract
|
April 2016 | Not Applicable |
| NCT03499873 | Actavis Inc. |
Cataract
|
March 28, 2018 | Phase 3 |
| NCT03886779 | Silverstein Eye Centers|Bausch & Lomb Incorporated|Churchhill Communications|Statistics & Data Corporation |
Treatment of Ocular Inflammation Associated With Cataract Surgery
|
October 30, 2013 | Phase 4 |
| NCT05331690 | Oslo University Hospital |
Cataract Surgery
|
May 2022 | Phase 4 |
| NCT02821390 | University Hospital of Patras |
Pain
|
June 2016 | Not Applicable |
| NCT02443012 | Universiti Sains Malaysia |
Diabetic Macular Edema
|
March 2013 | Phase 4 |
| NCT00939276 | Alcon Research |
Diabetic Retinopathy
|
August 2009 | Phase 3 |
| NCT01109173 | Alcon Research |
Cataract
|
June 2010 | Phase 3 |
| NCT03918590 | The New York Eye & Ear Infirmary |
Neovascular Age-related Macular Degeneration|Diabetic Macular Edema|Retinal Vein Occlusion
|
December 3, 2018 | Phase 4 |
| NCT03025945 | Intuor Technologies, Inc. |
Cystoid Macular Edema
|
October 2013 | Not Applicable |
| NCT00801905 | Asociación para Evitar la Ceguera en México |
Macular Thickening|Macular Edema
|
August 2008 | Phase 2 |
| NCT00405730 | Alcon Research |
Cataracts
|
November 2005 | Phase 3 |
| NCT00780780 | Federal University of São Paulo |
Diabetic Macular Edema
|
July 2007 | Phase 3 |
| NCT02506348 | Wolfson Medical Center |
Post Surgical Management|Pain Management|Inflamation Management
|
July 2015 | Not Applicable |
| NCT01310127 | Toyos Clinic|Bausch & Lomb Incorporated |
Inflammation|Pseudophakia
|
November 2010 | Phase 4 |
| NCT02361645 | Università degli Studi di Brescia |
Vitreous Inflammation
|
March 2014 | Phase 3 |
| NCT01001806 | Frank A. Bucci, Jr., M.D.|Allergan|Bucci Laser Vision Institute |
Cataracts
|
October 2009 | Phase 4 |
| NCT00330798 | Alcon Research|Matthew Caldwell |
Photorefractive Keratectomy
|
February 2006 | Phase 4 |
| NCT01995890 | Dr T V Patel Eye Institute |
Intraocular Pressure
|
December 2012 | Phase 4 |
| NCT01939691 | University of California, San Francisco|Aravind Eye Hospitals, India |
Uveitis|Macular Edema
|
September 12, 2018 | Phase 4 |
| NCT00407017 | Innovative Medical |
Cataract Surgery
|
Phase 4 | |
| NCT01021761 | Frank A. Bucci, Jr., M.D.|Allergan|Bucci Laser Vision Institute |
Cataracts
|
October 2009 | Phase 4 |
| NCT01331005 | Jaeb Center for Health Research|National Eye Institute (NEI) |
Diabetic Macular Edema
|
May 2011 | Phase 2 |
| NCT00818844 | Alcon Research |
Epiretinal Membrane
|
January 2009 | Phase 4 |
| NCT01426854 | Alcon Research |
Cataract
|
July 2011 | Phase 3 |
| NCT03496467 | Mati Therapeutics Inc. |
Pain|Inflammation
|
March 5, 2018 | Phase 2 |
| NCT01395069 | Queen´s University |
Macular Edema
|
February 2010 | Phase 4 |
| NCT01872611 | Alcon Research |
Non-Proliferative Diabetic Retinopathy|Cataract
|
June 2013 | Phase 3 |
| NCT05542381 | Virginia Polytechnic Institute and State University|Vistar Eye Center |
Age-Related Macular Degeneration
|
October 1, 2022 | Not Applicable |
| NCT00494494 | University of North Carolina, Chapel Hill|Research to Prevent Blindness |
Cystoid Macular Edema
|
June 2007 | Phase 4 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL ( 393.27 mM ; Need ultrasonic)
Preparing
Stock Solutions
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.9327 mL | 19.6634 mL | 39.3267 mL |
| 5 mM | 0.7865 mL | 3.9327 mL | 7.8653 mL |
| 10 mM | 0.3933 mL | 1.9663 mL | 3.9327 mL |
*
Please refer to the solubility information to select the appropriate solvent.
References
- [1] Gamache DA, Graff G, Brady MT et al. Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: I. Assessment of anti-inflammatory efficacy. Inflammation. 2000 Aug;24(4):357-70.
- [2] Ke TL, Graff G, Spellman JM, Yanni JM. Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: II. In vitro bioactivation and permeation of external ocular barriers. Inflammation. 2000 Aug;24(4):371-84.
- [3] Lindstrom R, Kim T. Ocular permeation and inhibition of retinal inflammation: an examination of data and expert opinion on the clinical utility of nepafenac. Curr Med Res Opin. 2006 Feb;22(2):397-404.
- [4] Marshall JC, Fernandes BF, Di Cesare S et al. The use of a cyclooxygenase-2 inhibitor (Nepafenac) in an ocular and metastatic animal model of uveal melanoma. Carcinogenesis. 2007 Sep;28(9):2053-8.
- [5] Singh R, Alpern L, Jaffe GJ et al. Evaluation of nepafenac in prevention of macular edema following cataract surgery in patients with diabetic retinopathy. Clin Ophthalmol. 2012;6:1259-69.
Synonyms
Benzeneacetamide, 2-amino-3-benzoyl-
2-Amino-3-benzoylbenzeneacetamide
AL 6515
Nepafenac
AHR 9434
Nevanac
Ilevro
2-(2-Amino-3-benzoylphenyl)acetamide
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