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SML2770

GSK2795039

Name: GSK2795039
Brand: SIGMA

≥98% (HPLC), NOX2 inhibitor, powder

别名:

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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关于此项目

经验公式（希尔记法）:

C₂₃H₂₆N₆O₂S

化学文摘社编号:

1415925-18-6

分子量:

450.56

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD30489720

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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属性

产品名称

GSK2795039, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

SMILES string

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

InChI key

FMWVTCZKCXPKFW-UHFFFAOYSA-N

说明

Biochem/physiol Actions

GSK2795039 is a non-cytotoxic (100μM, 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.

NADPH-competitive, potent and selective NOX2 inhibitor with in vitro and in vivo efficacy against NOX2-mediated ROS production and inflammation.

存储类别

11 - Combustible Solids

wgk

WGK 3

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Iron accentuated reactive oxygen species release by NADPH oxidase in activated microglia contributes to oxidative stress in vitro.

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

Crucial role for Nox2 and sleep deprivation in aircraft noise-induced vascular and cerebral oxidative stress, inflammation, and gene regulation.

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

NADPH Oxidase Mediates Membrane Androgen Receptor-Induced Neurodegeneration.

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

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全球贸易项目编号

货号	GTIN
SML2770-1MG	04061841693161
SML2770-5MG	04061841693178