Indomethacin

別名：Indometacin,NSC-77541

製品コード：S1723 純度：99.99%

Indomethacin is a nonselective COX1 and COX2 inhibitor with IC50 of 0.1 μg/mL and 5 μg/mL, respectively, used to reduce fever, pain, stiffness, and swelling.

CAS No. 53-86-1

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
50mg	JPY 22000	国内在庫あり
1g	JPY 55500	国内在庫あり

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（17）

カスタマーフィードバック1例

製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

Indomethacin関連製品

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関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Neuronal Signaling Compound Library CNS-Penetrant Compound Library Anti-alzheimer Disease Compound Library	もっと見る

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

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
THP1 cells	Function assay	100 μM	30 mins	Irreversible inhibition of COX-1 in human THP1 cells assessed as inhibition of arachidonic acid-induced TXB2 formation at 100 uM incubated for 30 mins followed by compound washout measured 30 mins post arachidonic acid challenge by radioimmunoassay	23651359
MDA-MB-231 cells	Function assay	100 μM	30 mins	Irreversible inhibition of COX-1 in human MDA-MB-231 cells assessed as inhibition of arachidonic acid-induced PGE2 formation at 100 uM incubated for 30 mins followed by compound washout measured 30 mins post arachidonic acid challenge by radioimmunoassay	23651359
LNCAP cells	Function assay	30 μM	48 h	Inhibition of AKR1C3 (unknown origin)-mediated testosterone-17beta-glucuronide formation expressed in human LNCAP cells at 30 uM after 48 hrs in presence of 4-androstene-3,17-dione	23432095
A549 cells	Function assay	10 μM		Inhibition of mPGES1 in human A549 cells assessed as inhibition of IL-1-beta-induced PGE2 formation at 10 uM by cell-intact assay	19053751
HepG2 cells	Function assay	100 μM		Inhibition of MRP1-mediated doxorubicin efflux in doxorubicin resistant human HepG2 cells at 100 uM by flow cytometry	20455578
HeLa cells	Function assay		20 mins	Agonist activity at androgen receptor (unknown origin) expressed in HeLa cells co-expressing PSA-(ARE)4-Luc13 assessed as induction of DHT-induced luciferase activity after 20 mins by luciferase reporter gene assay, EC50=0.14 nM	23432095
SF-9 insect cells	Function assay		20 Mins	Inhibition of human COX2 expressed in SF-9 insect cells assessed as conversion of [14C]-arachidonic acid to [14C]-prostaglandins preincubated for 20 mins by thin-layer chromatography analysis, IC50=0.75 μM	21524587
mouse RAW264.7 cells	Function assay		24 h	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess assay, IC50=1.25 μM	24806310
mouse BV2 cells	Function assay		24 h	Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess assay, IC50=7.1 μM	24042007
mouse BV2 cells	Cytotoxicity assay		24 h	Cytotoxicity against mouse BV2 cells assessed as maximum non-toxic concentration after 24 hrs by MTT assay	23711917
J774 cells	Function assay			In vitro inhibitory activity against Prostaglandin G/H synthase 1 in murine J774 cells, IC50=2 nM	15857149
U-937 cells	Function assay			In vitro inhibitory activity against human Prostaglandin G/H synthase 1 (COX-1) in U-937 cells, IC50=2 nM	12877584
rat synovial cells	Function assay			In vitro inhibitory effect on production of prostaglandin E2 (PGE2) in rat synovial cells, IC50=2.9 nM	10821716
143982 cells	Function assay			In vitro inhibitory activity against human Prostaglandin G/H synthase 2 (COX-2) in 143982 cells, IC50=9 nM	12877584
CHO cells	Function assay			In vitro inhibitory potency against human COX-1 in stably transfected chinese hamster ovary (CHO) cells, IC50=18 nM	10576684
RBL-1 cell line	Function assay			Inhibition of Prostaglandin G/H synthase in intact RBL-1 cell line, IC50=0.5 μM	2115586
human 2008 cells	Function assay			Inhibition of human MRP1 in human 2008 cells, IC50=12 μM	18707884
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Indomethacin is a nonselective COX1 and COX2 inhibitor with IC50 of 0.1 μg/mL and 5 μg/mL, respectively, used to reduce fever, pain, stiffness, and swelling.

Targets

COX1 ^[6]	COX-2 ^[6]
0.28 μM	14 μM

In Vitro
In vitro	Indomethacin inhibits transcription of a beta-catenin/TCF-responsive reporter gene in a dose dependent manner. Indomethacin also downregulates the beta-catenin/TCF transcriptional target cyclin D1. Indomethacin attenuates the transcription of beta-catenin/TCF-responsive genes, by modulating TCF activity without disrupting beta-catenin/TCF complex formation. ^[1]

In Vivo
In Vivo	Indomethacin increases BrdU⁺ cells of all lineages and reduces microglial/monocyte activation in rats after focal cerebral ischemia. ^[2] Indomethacin (7.5 mg/kg, one injection) produces acute injury and inflammation in the distal jejunum and proximal ileum that are maximal at three days and completely resolves within one week. Indomethacin (two daily subcutaneous injections) produces a more extensive and chronic inflammation that lasts in an active form in more than 75% of the rats for at least two weeks. ^[3] Indomethacin (4ppm) reduces tumor yield by 78% in SKH:HR-1-hrBr hairless mice. ^[4] Indomethacin (20 mg/kg, orally) increases the total area of gastric erosions and concentration of lipid peroxides in the gastric mucosa of rats. Indomethacin increases the alpha-tocopherol:total cholesterol ratio in serum. Indomethacin inhibits the increases in gastric mucosal erosions and lipid peroxides in the gastric mucosa, and the reduction of serum alpha-tocopherol. ^[5]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06031363	Completed	Pancreatitis\|Cholangiopancreatography Endoscopic Retrograde\|Indomethacin	The First Affiliated Hospital of Soochow University	November 1 2022	Not Applicable
NCT04821323	Completed	Healthy	Janssen Research & Development LLC	March 10 2021	Early Phase 1
NCT04025177	Withdrawn	Patent Ductus Arteriosus After Premature Birth	University of Manitoba\|St. Boniface Hospital\|Health Sciences Centre Winnipeg Manitoba\|University at Buffalo	January 2020	Phase 2
NCT03967483	Unknown status	Headache Migraine	Anne Ducros\|French Society for the Study of Migraine Headache	June 1 2019	--

参考
[1] Dihlmann S, et al. Oncogene, 2001, 20(5), 645-653. [2] Hoehn BD, et al. Stroke, 2005, 36(12), 2718-2724. [3] Yamada T, et al. Inflammation, 1993, 17(6), 641-662. [4] Fischer SM, et al. Mol Carcinog, 1999, 25(4), 231-240. [5] Yoshikawa T, et al. Gut, 1993, 34(6), 732-737. [6] Mitchell JA, et al. Proc Natl Acad Sci U S A. 1993, 90(24), 11693-11697. + 展開

参考

+ 展開

化学情報

分子量	357.79	化学式	C₁₉H₁₆ClNO₄
CAS No.	53-86-1	SDF	Download Indomethacin SDFをダウンロードする
Smiles	CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=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 : 72 mg/mL ( (201.23 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 : 24 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。

技術サポート

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