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Based on 1 Customer Validation
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.56%
- CAS 番号: 78281-72-8
- 分子式: C15H14N2O2
- 分子量:254.28
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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HY-B0577
Latanoprost
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HY-B0440
Tenoxicam
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HY-17357R
Nepafenac (Standard)
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HY-B0336
Pranoprofen
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HY-B0559
Nabumetone
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HY-14670
Firocoxib
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HY-B0336R
Pranoprofen (Standard)
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HY-B0440R
Tenoxicam (Standard)
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HY-B0559R
Nabumetone (Standard)
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HY-W251708
AHR 10240
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HY-14670R
Firocoxib (Standard)
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HY-B0577R
Latanoprost (Standard)
生物活性
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COX-1 64.3 μM (IC50) |
COX-2 0.12 μM (IC50) |
Nepafenac (0.05%-0.1% eye drops, 0-500 min) inhibits PGE₂ by 90-95% in the isolated rabbit iris/ciliary body and by 55% in the retina/choroid, for a duration of 6 hours and 4 hours, respectively at 1%[1].
Nepafenac (7-117 μM, 0-400 min) has a stronger isolated rabbit corneal and conjunctiva/sclera permeability than Diclofenac (HY-15036) with permeation coefficients (kps) of 727 × 10-6 min-1 and 128 × 10-6 min-1, respectively[2].
Nepafenac (0.05%-0.1% eye drops, 5 min) results in sustained flux of drug across the cornea for 6 h with short term perfusion of the isolated rabbit corneal surface and accumulates at 16.7 μM on the corneal endothelial side[2].
Nepafenac (8.9-140 μM, 0-6 h) can effectively hydrolyze into Amfenac in the cornea, iris/ciliary body, and retina/choroid of both rabbit and human eyes, moreover, the hydrolysis in rabbit cornea shows time and dose dependence[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Nepafenac (0.3% eye drops, topical ocular administration, twice daily for 12 weeks) delays the progression of uveal melanoma (UM) in rabbits[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Trauma-induced model of acute ocular inflammation established in New Zealand Albino rabbits (2-2.5 kg)[1]
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Dosage:0.1% eye drops
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Administration:Topical ocular administration, single dose
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Result:Reduced protein exudation by 61% and inhibited PGE₂ by 98%. Exhibited the anti-inflammatory effect lasts for 8 hours after a single administration.
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Animal Model:Human UM cell line induced xenograft tumor model established in male New Zealand albino rabbits[3]
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Dosage:0.3% eye drops
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Administration:Topical ocular administration, twice daily for 12 weeks
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Result:Reduced the incidence of tumors.
Alleviated the tumor morphology, mainly presenting as flat lesions (in the control group, large tumors accompanied by vitreous hemorrhage were more common).
Significantly reduced the staining intensity of COX-2 in tumors. Delayed the appearance time of circulating tumor cells (CMCs), and reduced the lung and liver metastasis of the tumor.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 78281-72-8
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性状 Solid
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分子量 254.28
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分子式 C15H14N2O2
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Color Light yellow to yellow
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SMILES
O=C(N)CC1=CC=CC(C(C2=CC=CC=C2)=O)=C1N
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別名
Nepafenac; AHR 9434; AL 6515
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
溶剤 & 溶解度
DMSO : 100 mg/mL (393.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (275 KB)
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SDS (398 KB)
- English - EN (398 KB)
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- Deutsch - DE (398 KB)
- Norwegian - NO (398 KB)
- Español - ES (398 KB)
- Swedish - SV (398 KB)
- Italian - IT (398 KB)
- Korean - KR (398 KB)
- Portuguese - PT (398 KB)
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取扱説明書 (2659 KB)
参考文献
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.9327 mL | 19.6634 mL | 39.3267 mL | 98.3168 mL |
| 5 mM | 0.7865 mL | 3.9327 mL | 7.8653 mL | 19.6634 mL | |
| 10 mM | 0.3933 mL | 1.9663 mL | 3.9327 mL | 9.8317 mL | |
| 15 mM | 0.2622 mL | 1.3109 mL | 2.6218 mL | 6.5545 mL | |
| 20 mM | 0.1966 mL | 0.9832 mL | 1.9663 mL | 4.9158 mL | |
| 25 mM | 0.1573 mL | 0.7865 mL | 1.5731 mL | 3.9327 mL | |
| 30 mM | 0.1311 mL | 0.6554 mL | 1.3109 mL | 3.2772 mL | |
| 40 mM | 0.0983 mL | 0.4916 mL | 0.9832 mL | 2.4579 mL | |
| 50 mM | 0.0787 mL | 0.3933 mL | 0.7865 mL | 1.9663 mL | |
| 60 mM | 0.0655 mL | 0.3277 mL | 0.6554 mL | 1.6386 mL | |
| 80 mM | 0.0492 mL | 0.2458 mL | 0.4916 mL | 1.2290 mL | |
| 100 mM | 0.0393 mL | 0.1966 mL | 0.3933 mL | 0.9832 mL |
Nepafenac 関連分類
HY-17357 関連分類
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