78281-72-8
78281-72-8
Chemical Structure
Nepafenac
Synonym(s): AHR 9434; AL 6515
- CAS No.: 78281-72-8
- Formula:C15H14N2O2
- Molecular Weight:254.28
IUPAC Name: 2-(2-amino-3-benzoylphenyl)acetamide
InChIKey: QEFAQIPZVLVERP-UHFFFAOYSA-N
SMILES: O=C(N)CC1=CC=CC(C(C2=CC=CC=C2)=O)=C1N
Biological Activity: Nepafenac (AHR 9434; AL 6515), a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC50 of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC50 = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Nepafenac | 99.56% | Nepafenac (AHR 9434; AL 6515), a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC50 of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC50 = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries. | ||||||||||||||||||||
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Nepafenac (Standard) | ≥98% | Nepafenac (AHR 9434; AL 6515) (Standard) is the analytical standard of Nepafenac (HY-17357). This product is intended for research and analytical applications. Nepafenac, a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC50 of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC50 = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries. | ||||||||||||||||||||
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Nepafenac-d5 | 98.84% | Nepafenac-d5 (AHR-9434-d5; AL-6515-d5) is the deuterium labeled Nepafenac (HY-17357). Nepafenac, a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC50 of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC50 = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries. | ||||||||||||||||||||
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AHR-6293 | AHR-6293 is an orally effective and potent anti-inflammatory agent. AHR-6293 has a better anti-inflammatory effect than AHR-5850, but does not have the activity of inhibiting platelet aggregation. | |||||||||||||||||||||
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AHR-10037 | AHR-10037 is a non-steroidal anti-inflammatory agent with low gastric toxicity. AHR-10037 is a prodrug converted in vivo to a cyclooxygenase inhibitor. | |||||||||||||||||||||
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Desmethyl Ketoprofen | 97.0% | Desmethyl Ketoprofen has anti-inflammatory activities. Desmethyl Ketoprofen can be used for the study of angiogenesis-related disorders. | ||||||||||||||||||||
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5-Hydroxynepafenac-d5 | 5-Hydroxynepafenac-d5 is deuterium-labeled 5-Hydroxynepafenac. | |||||||||||||||||||||
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Amfenac | Amfenac (AHR 5850) is an orally active and potent anti-inflammatory compound possessing antipyretic and analgesic properties. Amfenac can be used for the research of acute and chronic inflammation. | |||||||||||||||||||||
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Amfenac Sodium Hydrate | 98.33% | Amfenac Sodium Hydrate is a COX-2 inhibitor. | ||||||||||||||||||||
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Amfenac sodium | Amfenac sodium (AHR 5850 sodium) is an orally active and potent anti-inflammatory compound possessing antipyretic and analgesic properties. Amfenac sodium can be used for the research of acute and chronic inflammation. | |||||||||||||||||||||
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Amfenac-d5 | Amfenac-d5 is the deuterium labeled Amfenac. Amfenac is an orally active and potent anti-inflammatory compound possessing antipyretic and analgesic properties. Amfenac can be used for the research of acute and chronic inflammation. | |||||||||||||||||||||
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Amfenac ethyl ester | Amfenac ethyl ester is an orally active cyclooxygenase (COX) inhibitor. Amfenac ethyl ester exhibits antiinflammatory activity in rodent models. Amfenac ethyl ester can be used for the research of inflammation. | |||||||||||||||||||||
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2-Amino-5-Chlorobenzophenone-d5 | 2-Amino-5-Chlorobenzophenone-d5 is the deuterium labeled 2-Amino-5-Chlorobenzophenone. | |||||||||||||||||||||
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Oxybenzone-d5 | 99% | Oxybenzone-d5 is the deuterium labeled Oxybenzone. Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells. | ||||||||||||||||||||
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Bromfenac | Bromfenac is a potent and orally active inhibitor of COX, with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac can be used in ocular inflammation research. | |||||||||||||||||||||
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Bromfenac sodium | 99.92% | Bromfenac sodium is a potent and orally active inhibitor of COX, with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac sodium can be used in ocular inflammation research. | ||||||||||||||||||||
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Bromfenac-d4 sodium | Bromfenac-d4 (sodium) is deuterium labeled Bromfenac (sodium). Bromfenac sodium is a potent and orally active inhibitor of COX, with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac sodium is a brominated non-steroidal anti-inflammatory/analgesic agent (NSAID), and it is commonly used for the research of postoperative inflammation and pain following cataract surgery, and pseudophakic cystoid macular edema (CME). | |||||||||||||||||||||
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2-Amino-5-nitrobenzophenone-d5 | 2-Amino-5-nitrobenzophenone-d5 is the deuterium labeled 2-Amino-5-nitrobenzophenone. | |||||||||||||||||||||
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(4-Nitrophenyl)(phenyl)methanone-d5 | (4-Nitrophenyl)(phenyl)methanone-d5 is the deuterium labeled (4-Nitrophenyl)(phenyl)methanone. | |||||||||||||||||||||
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2,4′-Dihydroxybenzophenone-d5 | (2,4-Dihydroxyphenyl)(phenyl)methanone-d5 is the deuterium labeled (2,4-Dihydroxyphenyl)(phenyl)methanone. | |||||||||||||||||||||
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Ketoprofen impurity 5 | Ketoprofen impurity 5 (rac Ketoprofen amide) is an impurity of Ketoprofen. | |||||||||||||||||||||
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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. [Content Brief]
- [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. [Content Brief]
- [3]. 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. [Content Brief]
