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Merck

SML2770

Sigma-Aldrich

GSK2795039

≥98% (HPLC)

別名:

GSK 2795039, GSK-2795039, N-(1-Isopropyl-3-(1-methylindolin-6-yl)-1H-pyrrolo[2,3-b]pyridin-4-yl)-1-methyl-1H-pyrazole-3-sulfonamide

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About This Item

実験式(ヒル表記法):
C23H26N6O2S
CAS番号:
分子量:
450.56
MDL番号:
UNSPSCコード:
12352200
NACRES:
NA.77

品質水準

アッセイ

≥98% (HPLC)

形状

powder

white to beige

溶解性

DMSO: 2 mg/mL, clear

保管温度

−20°C

SMILES記法

O=S(NC1=C2C(N(C(C)C)C=C2C3=CC4=C(C=C3)CCN4C)=NC=C1)(C5=NN(C)C=C5)=O

生物化学的/生理学的作用

GSK2795039 is a non-cytotoxic (100 μM, 24 hrs, HEK293), NADPH-competitive, potent and selective NOX2 inhibitor (IC50/[NADPH] = 447 nM/25 μM, 2.29 μM/1 mM by NADPH depletion measurement; eNOS & NOX1/3/4/5 IC50 >100 μM, PKCB II IC50 >25 μM, xanthine oxidase IC50 = 28.8 μM). GSK2795039 inhibits PMA-induced reactive oxygen species (ROS) production in cultures (IC50 = 182 nM; HL60) and exhibits in vivo efficacy against complete Freund′s adjuvant-induced paw inflammation (ED50 = 2 mg/kg, ED100 = 100 mg/kg ip.) as well as cerulein-induced acute pancreatitis (ED50 = 100 mg/kg ip.) in mice.

保管分類コード

11 - Combustible Solids

WGK

WGK 3


適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

Jan Code

SML2770-5MG:
SML2770-1MG:
SML2770-BULK:
SML2770-VAR:


試験成績書(COA)

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以前この製品を購入いただいたことがある場合

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Young J Yauger et al.
Journal of neuroinflammation, 16(1), 41-41 (2019-02-20)
Excessive iron contributes to oxidative stress after central nervous system injury. NADPH oxidase (NOX) enzymes are upregulated in microglia after pro-inflammatory activation and contribute to oxidative stress. The relationship between iron, microglia, NOX, and oxidative stress is currently unclear. We
Swenja Kröller-Schön et al.
European heart journal, 39(38), 3528-3539 (2018-06-16)
Aircraft noise causes endothelial dysfunction, oxidative stress, and inflammation. Transportation noise increases the incidence of coronary artery disease, hypertension, and stroke. The underlying mechanisms are not well understood. Herein, we investigated effects of phagocyte-type NADPH oxidase (Nox2) knockout and different
Mavis A A Tenkorang et al.
Endocrinology, 160(4), 947-963 (2019-02-28)
Oxidative stress (OS) is a common characteristic of several neurodegenerative disorders, including Parkinson disease (PD). PD is more prevalent in men than in women, indicating the possible involvement of androgens. Androgens can have either neuroprotective or neurodamaging effects, depending on
Shannon C Kelly et al.
Redox biology, 27, 101075-101075 (2018-12-24)
The reduction of extracellular oxidants by intracellular electrons is known as trans-plasma membrane electron transport (tPMET). The goal of this study was to characterize a role of tPMET in the sensing of glucose as a physiological signal. tPMET from C2C12
Kazufumi Hirano et al.
Antioxidants & redox signaling, 23(5), 358-374 (2015-07-03)
The NADPH oxidase (NOX) family of enzymes catalyzes the formation of reactive oxygen species (ROS). NOX enzymes not only have a key role in a variety of physiological processes but also contribute to oxidative stress in certain disease states. To

ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.

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