Nepafenac

製品コードS1255 バッチS125502

印刷

化学情報

Synonyms

AHR 9434, AL 6515

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₅H₁₄N₂O₂

分子量

254.28

CAS No.

78281-72-8

Solubility (25°C)*

体外

DMSO

51 mg/mL (200.56 mM)

Ethanol

4 mg/mL (15.73 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Nepafenac（AHR 9434、AL 6515）は、amfenacのプロドラッグであり、COX-1およびCOX-2活性の阻害剤として作用し、白内障手術に伴う痛みと炎症の治療に使用されます。
in vivo	Nepafenac shows significantly greater ocular bioavailability and amfenac demonstrated greater potency at COX-2 inhibition than ketorolac or bromfenac. This compound exhibits only weak COX-1 inhibitory activity with IC50 of 64.3 mM. It inhibits prostaglandin synthesis in the iris/ciliary body (85-95%) and the retina/choroid (55%) in rabbits. This chemical (0.5%) produces 65% reduction in retinal edema which is correlated with 62% inhibition of blood-retinal barrier breakdown. It (0.5%) significantly inhibits (46%) blood-retinal barrier breakdown concomitant with near total suppression of PGE2 synthesis (96%). It significantly inhibits retinal prostaglandin E(2), superoxide, cyclooxygenase-2, and leukostasis within retinal microvessels in insulin-deficient diabetic rats, without affecting vascular endothelial growth factor (VEGF) and nitric oxide (NO). This compound significantly inhibits the number of transferase-mediated dUTP nick-end labeling-positive capillary cells, acellular capillaries, and pericyte ghosts in diabetic rats. It results in significantly less choroidal neovascularization and significant less ischemia-induced retinal neovascularization in mice compare to control. This chemical also blunts the increase in VEGF mRNA in the retina induced by ischemia. It delays the progression of malignancy as well as reduces weight in an ocular and metastatic animal model of uveal melanoma.

製品説明

Nepafenac（AHR 9434、AL 6515）は、amfenacのプロドラッグであり、COX-1およびCOX-2活性の阻害剤として作用し、白内障手術に伴う痛みと炎症の治療に使用されます。

in vivo

Nepafenac shows significantly greater ocular bioavailability and amfenac demonstrated greater potency at COX-2 inhibition than ketorolac or bromfenac. This compound exhibits only weak COX-1 inhibitory activity with IC50 of 64.3 mM. It inhibits prostaglandin synthesis in the iris/ciliary body (85-95%) and the retina/choroid (55%) in rabbits. This chemical (0.5%) produces 65% reduction in retinal edema which is correlated with 62% inhibition of blood-retinal barrier breakdown. It (0.5%) significantly inhibits (46%) blood-retinal barrier breakdown concomitant with near total suppression of PGE2 synthesis (96%). It significantly inhibits retinal prostaglandin E(2), superoxide, cyclooxygenase-2, and leukostasis within retinal microvessels in insulin-deficient diabetic rats, without affecting vascular endothelial growth factor (VEGF) and nitric oxide (NO). This compound significantly inhibits the number of transferase-mediated dUTP nick-end labeling-positive capillary cells, acellular capillaries, and pericyte ghosts in diabetic rats. It results in significantly less choroidal neovascularization and significant less ischemia-induced retinal neovascularization in mice compare to control. This chemical also blunts the increase in VEGF mRNA in the retina induced by ischemia. It delays the progression of malignancy as well as reduces weight in an ocular and metastatic animal model of uveal melanoma.

プロトコル(参考用のみ)

参考

https://pubmed.ncbi.nlm.nih.gov/10850857/
https://pubmed.ncbi.nlm.nih.gov/10850857/
https://pubmed.ncbi.nlm.nih.gov/14635785/

https://pubmed.ncbi.nlm.nih.gov/17259381/
https://pubmed.ncbi.nlm.nih.gov/12506103/
https://pubmed.ncbi.nlm.nih.gov/17434930/

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

KEAP1 Mutations Drive Tumorigenesis by Suppressing SOX9 Ubiquitination and Degradation [ Adv Sci (Weinh), 2020, 7(21):2001018]	PubMed: 33173725

KEAP1 Mutations Drive Tumorigenesis by Suppressing SOX9 Ubiquitination and Degradation [ Adv Sci (Weinh), 2020, 7(21):2001018]

PubMed: 33173725

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。