1400W 2HCl

別名:N-(3-(Aminomethyl)benzyl)acetamidine

1400W (N-(3-(Aminomethyl)benzyl)acetamidine) is a slow, tight binding, and highly selective inhibitor of inducible nitric-oxide synthase(iNOS).

1400W 2HCl化学構造

CAS No. 214358-33-5

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 59500 国内在庫あり
JPY 149500 国内在庫あり
JPY 448500 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]
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1400W 2HCl関連製品

NOS阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
RAW264.7 Antiinflammatory assay 50 uM 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite production at 50 uM treated 30 mins before LPS challenge measured after 24 hrs by Griess method 20447741
RAW264.7 Antiinflammatory assay 0.5 to 2 uM 2 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced COX-2 expression at 0.5 to 2 uM incubated for 2 hrs prior to LPS challenge measured after 24 hrs by Western blot analysis 23232148
RAW264.7 Antiinflammatory assay 2 uM 2 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as downregulation of LPS-induced iNOS mRNA expression at 2 uM incubated for 2 hrs prior to LPS challenge measured after 9 hrs by RT-PCR analysis 23232148
RAW264.7 Antiinflammatory assay 0.5 to 2 uM 2 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced iNOS expression at 0.5 to 2 uM incubated for 2 hrs prior to LPS challenge measured after 24 hrs by Western blot analysis 23232148
RAW264.7 Function assay 4 uM Inhibition iNOS mRNA expression levels in LPS-induced mouse RAW264.7 cells at 4 uM by RT-PCR analysis 27542306
RAW264.7 Function assay 4 uM Inhibition iNOS protein expression levels in LPS-induced mouse RAW264.7 cells at 4 uM by Western blot analysis 27542306
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50=0.2μM 23232148
RAW264.7 Antiinflammatory assay 20 hrs Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as nitrite accumulation after 20 hrs by fluorimetry, IC50=0.3μM 11678654
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite accumulation after 24 hrs, IC50=2.9μM 15568764
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as effect on NO production pretreated 1 hr before LPS challenge measured after 24 hrs, IC50=3.1μM 11908984
RAW 264 Function assay 24 hrs Inhibition of 1ug/ml LPS-stimulated nitirc oxide accumulation in RAW 264 cells after 24 hrs, IC50=5.2μM 17320246
N9 Antiinflammatory assay 24 hrs Antiinflammatory activity against mouse N9 cells assessed as inhibition of LPS/IFN-gamma-induced nitrite accumulation after 24 hrs, IC50=6.3μM 15568764
RAW264.7 Cytotoxicity assay 24 hrs Cytotoxicity against mouse RAW264.7 cells assessed as cell viability after 24 hrs by MTS assay, IC50=47.47μM 23232148
RAW264.7 Function assay Inhibition of LPS-induced nitric oxide generation in mouse RAW264.7 cells pretreated 1 hr before LPS challenge by Griess method, IC50=1.5μM 19278854
N9 Function assay Inhibitory effect of compound on the accumulation of NO2 in the culture media of N9 cells in response to LPS/IFN-gamma, IC50=2.2μM 15013012
RAW264.7 Antiinflammatory assay Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production pretreated 1 hr before LPS challenge, IC50=2.3μM 12662101
RAW264.7 Function assay Inhibition of LPS-induced nitric oxide accumulation in mouse RAW264.7 cells, IC50=2.7μM 19699097
N9 Antiinflammatory assay Antiinflammatory activity in LPS/IFN-gamma-stimulated mouse N9 cells assessed as inhibition of nitric oxide production pretreated 1 hr before LPS/IFNgamma challenge, IC50=3.6μM 12662101
RAW264.7 Function assay Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells, IC50=3.78μM 17988874
RAW264.7 Function assay Inhibitory effect of compound on the accumulation of NO2 in the culture media of RAW 264.7 cells in response to LPS, IC50=6.1μM 15013012
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生物活性

製品説明 1400W (N-(3-(Aminomethyl)benzyl)acetamidine) is a slow, tight binding, and highly selective inhibitor of inducible nitric-oxide synthase(iNOS).
Targets
iNOS [1]
(Cell-free assay)
nNOS [1]
(Cell-free assay)
eNOS [1]
(Cell-free assay)
<7 nM(Kd) 2 μM(Ki) 50 μM(Ki)
In Vitro
In vitro 1400W is either an irreversible inhibitor or an extremely slowly reversible inhibitor of human iNOS. Inhibition of human iNOS by 1400W is time-dependent. 1400W is competitive with L-arginine. 1400W is not a substrate for iNOS[1].
細胞実験 細胞株 RAW264.7 cells
濃度 100 μM
反応時間 16 h
実験の流れ RAW264.7 cells are treated with LPS/IFNγ for 16 h and GAPDH-p300 binding is abolished by the iNOS inhibitor 1400W (100 μM). Cell lysates are immunoprecipitated with an anti-p300 antibody and the immunoprecipitates are analysed by western blotting with an anti-GAPDH antibody.
In Vivo
In Vivo 1400W selectively prevents microvasculature injury in rats. 1400W is greater than 50-fold more potent against iNOS than eNOS in a rat model of endotoxin-induced vascular injury. Moreover, 1400W also dose-dependently reduces LPS-induced vascular leakage associated with iNOS induction in the colon, lung, liver, kidney, and heart. The maximal protection is close to 100% for all organs except the kidney (kidney:54%)[1]. 1400W has an ameliorative effect on both oxidative and nitrosative stress in the kidneys against renal I/R injury in rats[2]. Treatment with 1400W can reduce the rate of growth of solid tumors in mice[4].
動物実験 動物モデル Rats
投与量 0.1-10 mg/kg
投与経路 s.c.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00845169 Completed
Endothelial Dysfunction
University of Edinburgh|NHS Lothian|Umeå University
April 2012 Not Applicable

化学情報

分子量 250.17 化学式

C10H15N3.2HCl

CAS No. 214358-33-5 SDF Download 1400W 2HCl SDFをダウンロードする
Smiles CC(=NCC1=CC=CC(=C1)CN)N.Cl.Cl
保管

In vitro
Batch:

DMSO : 35 mg/mL ( (139.9 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。)

Water : 35 mg/mL

Ethanol : 35 mg/mL

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

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)

mg/kg g μL

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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Handling Instructions

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