Ibuprofen (NSC 256857)

別名：Dolgesic,NSC 256857

製品コード：S1638 純度：100%

Ibuprofen (NSC 256857, Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively.

CAS No. 15687-27-1

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 23500	国内在庫あり
50mg	JPY 18100	国内在庫あり
1g	JPY 101400	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（7）

製品安全説明書

現在のバッチを見る： S163801 DMSO] 41 mg/mL] false] Ethanol] 41 mg/mL] false] Water] Insoluble] false 純度： 100%

100

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シグナル伝達経路

COXシグナル伝達経路

COX阻害剤の選択性比較

生物活性

製品説明

Ibuprofen (NSC 256857, Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively.

特性

Considered a core medicine in the WHO's "WHO Model List of Essential Medicines" (a list of the minimum medical requirements for a basic healthcare system).

Targets

COX-1 ^[1]	COX-2 ^[1]
13 μM	370 μM

In Vitro
In vitro	Ibuprofen works by inhibiting the enzyme cyclooxygenase COX-1 and COX-2, which convert arachidonic acid to prostaglandin H2 (PGH2). Its action is similar to aspirin, indomethacin and all other NSAIDs in intact cells, broken cells, and purified enzyme preparations. ^[1] Ibuprofen inhibits the constitutive activation of NF-κB and IKKα in the androgen-independent prostate tumor cells PC-3 and DU-145. It sensitizes prostate cells to ionizing radiation and blocks stimulated activation of NF-κB following exposure to TNFα or ionizing radiation in the androgen-sensitive prostate tumor cell line LNCaP. Both of these cannot be attributed directly to inhibition of IκB-α kinase but to inhibition of an upstream regulator of IKKα. ^[2] Ibuprofen exerts an anticancer effect by reducing survival of cancer cells. Ibuprofen is more efficacious than aspirin and acetaminophen, and comparable with (R)-flurbiprofen and indomethacin in induction of p75^NTR protein (a tumor and metastasis suppressor) expression in cell lines from bladder and other organs. ^[3]
Kinase Assay	Radiochemical enzyme assays for COX-1 and COX-2
Kinase Assay	10 μL of purified COX-1 (0.7-0.8 μg) or COX-2 (3.0 units, 0.3μg) is activated with 50 μL of cofactor solution [l-epinephrine (1.3 mg/mL), reduced glutathione (0.3 mg/mL), and hematin (1.3 mg/mL) in oxygen-free Tris-HCl buffer (pH 8.0)]. The enzyme solution (60 μL) is added to Ibuprofen solutions or DMSO (20 μL) after [¹⁴C]arachidonic acid is added in 0.2 mL eight-strip test tubes and preincubated 10 minutes on ice. Samples are incubated for 15 minutes at 37 °C, after which the reaction is terminated by addition of 10 μL of 2 M HCl and 5 μL of carrier solution (PGE2 and PGF2α, 0.2 μg/mL of each in EtOH). The unmetabolized arachidonic acid is separated from the prostaglandin products by column chromatography and eluted with n-hexane-dioxane-glacial acetic acid (70:30:1). The prostaglandin products are then eluted with EtOAc-MeOH (85:15), and the samples are counted in a Packard scintillation spectrometer. IC50 values are obtained by linear regression analysis.
細胞実験	細胞株	Bladder epithelial cell line T24, RT-4 transitional cell papilloma bladder cell line, 5637 primary carcinoma bladder cell line, HCT-116, MDAMB231, MCF7, HEK293, A549, SKOV3 and DU145
	濃度	Dissolved in DMSO at a concentration of 200 mM for making the stock solution, final concentration ~2 mM
	反応時間	48 hours
	実験の流れ	Each cell line is incubated with Ibuprofen of various concentrations for 48 hours. Cell survival is estimated by the MTT assay, and cell death is determined by Hoechst staining used to distinguish between intact cell nuclei and fragmented nuclei undergoing cell death. Cells are lysed and analyzed by western blotting for detection of the p75^NTR protein.

In Vivo
In Vivo	Ibuprofen reacts with the heme group of cyclooxygenase to prevent arachidonic acid conversion. Prior exposure to Ibuprofen in vivo protects cyclooxygenase completely from the irreversible effects of aspirin in platelets. ^[4] Ibuprofen treatment is effective in attenuating joint inflammation and early articular cartilage degeneration in the adult female Sprague-Dawley rat model induced by high-repetition and high-force (HRHF) task. It dose this by blocking the increases in serum C1 and 2C (a biomarker of collagen I and II degradation) as well as the ratio of collagen degradation to synthesis (C1, 2C/CPII, the latter a biomarker of collage type II synthesis) induced by HRHF. ^[5]
動物実験	動物モデル	Female Sprague-Dawley rats with joint inflammation induced by high-repetition and high-force (HRHF) tasks
	投与量	45 mg/kg
	投与経路	Taken orally every day

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06146491	Recruiting	Pain Postoperative	B.P. Koirala Institute of Health Sciences	August 10 2023	Phase 4
NCT05928520	Not yet recruiting	Pain Management	Al-Azhar University	August 1 2023	Phase 3
NCT06247462	Completed	Acute Kidney Injury	University of New Mexico	June 1 2023	Phase 1
NCT05575700	Recruiting	Pain Acute\|Hip Arthropathy\|Knee Arthropathy\|Safety Issues\|Analgesia\|Analgesic Adverse Reaction\|Postoperative Pain\|Postoperative Complications	Naestved Hospital	April 17 2023	Phase 4
NCT05496868	Recruiting	Acute Respiratory Distress Syndrome Adult	Dompé Farmaceutici S.p.A	February 7 2023	Phase 2

参考
[1] Noreen Y, et al. J Nat Prod, 1998, 61(1), 2-7. [2] Palayoor ST, et al. Oncogene, 1999, 18(51), 7389-7394. [3] Khwaja F, et al. Cancer Res, 2004, 64(17), 6207-6213. [4] Rao GH, et al. Arteriosclerosis, 1983, 3(4), 383-388. [5] Driban JB, et al. J Biomed Biotechnol, 2011, 2011, 691412-691428. + 展開

参考

+ 展開

化学情報

分子量	206.28	化学式	C₁₃H₁₈O₂
CAS No.	15687-27-1	SDF	Download Ibuprofen (NSC 256857) SDFをダウンロードする
Smiles	CC(C)CC1=CC=C(C=C1)C(C)C(=O)O
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 41 mg/mL ( (198.75 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 41 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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