GKT136901 hydrochloride

A dual inhibitor of NOX1 and NOX4

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
5mg

￥550.00

440.00

- +
10mg

￥812.00

650.00

- +
25mg

￥1525.00

1220.00

- +
50mg

￥2175.00

1740.00

- +
100mg

￥3050.00

2440.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

货号: ajcx34804
CAS: 1254507-01-1
别名:
分子式: C19H16Cl2N4O2
分子量: 403.26
纯度: >98%
溶解度: DMSO : 62.5 mg/mL (154.99 mM; Need ultrasonic)|Water : 4 mg/mL (9.92 mM; ultrasonic and warming and heat to 60°C)
储存: Store at -20°C
库存: 现货

Background

GKT136901 is a dual inhibitor of NADPH oxidase 1 (NOX1) and NOX4 (K_is = 160 and 165 nM, respectively).¹ It is selective for NOX1 and NOX4 over NOX2 and xanthine oxidase (K_is = 1,530 and >30,000 nM, respectively), as well as over a panel of 18 enzymes and ion channels at 10 ?M. GKT136901 (0.1, 1, and 10 ?M) scavenges peroxynitrite radicals, as well as prevents the nitration and dimerization of α-synuclein, in cell-free assays.² It prevents peroxynitrite-induced cell death of differentiated LUHMES cells when used at a concentration of 10 ?M.

1.Laleu, B., Gaggini, F., Orchard, M., et al.First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosisJ. Med. Chem.53(21)7715-7730(2010) 2.Schildknecht, S., Weber, A., Gerding, H.R., et al.The NOX1/4 inhibitor GKT136901 as selective and direct scavenger of peroxynitriteCurr. Med. Chem.21(3)365-376(2014)