GKT136901
目录号: PL01237 纯度: ≥99%
CAS No. :955272-06-7
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中文名称
GKT136901
中文别名
2-(2-氯苯基)-4-甲基-5-(吡啶-2-基甲基)-1H-吡唑并[4,3-c]吡啶-3,6(2H,5H)-二酮
英文名称
GKT136901
英文别名
2-(2-Chlorophenyl)-4-methyl-5-(pyridin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;AK120765;GKT136901;2-(2-Chlorophenyl)-4-methyl-5-(2-pyridinylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione (ACI);GKT 136901
Cas No.
955272-06-7
分子式
C19H15ClN4O2
分子量
366.80
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
GKT136901 是一种有效的,选择性的和具有口服活性的 NADPH 氧化酶 NOX-1/4 抑制剂,Ki 值分别为 160 和 165 nM。GKT136901 也是一种选择性和直接的过氧亚硝酸清除剂。GKT136901 可用于糖尿病肾病,中风和神经退行性疾病的研究。GKT136901 还具有抗炎症活性。
生物活性
GKT136901 is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with K i s of 160 and 165 nM, respectively. GKT136901 is also a selective and direct scavenger of peroxynitrite. GKT136901 can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 also has anti-inflammatory activity.
性状
Solid
IC50 & Target[1][2]
Ki: 160 (NOX1), 165 (NOX4)
体外研究(In Vitro)
GKT136901 (10 μM; 30 min) significantly attenuates high-D-glucose-induced increase in O2 production and in H2O2 generation in MPT cells.
GKT136901 (10 μM; 30 min) abolishes the effect of high D-glucose on p38MAP kinase activation in MPT cells.
GKT136901 (10 μM; 2 h) attenuates methamphetamine (METH)-induced oxidative stress in HBMECs.
GKT136901 (10 μM; 2 h) protects HBMECs against METH-induced blood-brain barrier (BBB) dysfunction. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
GKT136901 (30-90 mg/kg; daily p.o. for 16 weeks) has renoprotective effects in a mouse model of Type 2 diabetes. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male db/db and
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Laleu B, et, al. First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis. J Med Chem. 2010 Nov 11;53(21):7715-30.
[2]. Teixeira G, et, al. Therapeutic potential of NADPH oxidase 1/4 inhibitors. Br J Pharmacol. 2017 Jun;174(12):1647-1669.
溶解度数据
In Vitro: DMSO : 33.33 mg/mL (90.87 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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