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| 商品编号 | 规格 | 价格 | 会员价 | 是否有货 | 数量 |
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| PL02585-2mg | 2mg | ¥1173.00 | 请登录 |
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| PL02585-5mg | 5mg | ¥1768.00 | 请登录 |
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| PL02585-10mg | 10mg | ¥2973.00 | 请登录 |
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| PL02585-50mg | 50mg | ¥9643.00 | 请登录 |
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| PL02585-100mg | 100mg | ¥13018.00 | 请登录 |
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| PL02585-200mg | 200mg | 询价 | 询价 |
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| PL02585-500mg | 500mg | 询价 | 询价 |
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| PL02585-10mM*1mLinDMSO | 10mM*1mLinDMSO | ¥1536.00 | 请登录 |
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| 中文名称 |
Setanaxib
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|---|---|
| 中文别名 |
2-(2-氯苯基)-4-[3-(二甲基氨基)苯基]-5-甲基-1H-吡唑并[4,3-c]吡啶-3,6(2H,5H)-二酮;2-(2-氯苯基)-4-(3-(二甲氨基)苯基)-5-甲基-1H-吡唑并[4,3-c]吡啶-3,6(2H,5H)-二酮;GKT137831 抑制剂
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| 英文名称 |
Setanaxib
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| 英文别名 |
2-(2-Chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;GKT-137831;2-(2-chlorophenyl)-4-[3-(dimethylamino)phenyl]-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6-dione;GKT137831;2-(2-Chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1H-pyrazolo(4,3-c)pyridine-3,6(2H,5H)-dione;AK134876;SureCN1302603;UNII-45II35329V;Setanaxib;45II35329V;GKT 137831;setanaxib (proposed INN);GTPL9932;GKT831;AOB5773;BCP14159
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| Cas No. |
1218942-37-0
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| 分子式 |
C21H19ClN4O2
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| 分子量 |
394.85
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| 包装储存 |
Powder -20°C 3 years；4°C 2 years
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| 产品详情 |
Setanaxib (GKT137831) 是选择性的NADPH氧化酶 (NOX1/4) 抑制剂，Ki 分别为140和110nM。
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|---|---|
| 生物活性 |
Setanaxib (GKT137831) is a selective NADPH oxidase (NOX1/4) inhibitor with K i s of 140 and 110 nM, respectively.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
Ki: 140±40 nM (Nox1), 1750±700 nM (Nox2), 110±30 nM (Nox4), 410±100 nM(Nox5)
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| 体外研究(In Vitro) |
Setanaxib (GKT137831) is a potent Nox1/4 inhibitor (Kis=140±40/110±30 nM). Administration of Setanaxib (GKT137831) throughout the 72-hour period of normoxia or hypoxia exposure attenuates HPASMC proliferation under normoxic conditions at the 20 μM concentration but had no effect on proliferation in normoxic HPAECs. In the prevention paradigm, Setanaxib (GKT137831) attenuates hypoxia-induced HPASMC and HPAEC proliferation at 5 and 20 μM. Complementary assays of cell proliferation measuring the expression of PCNA or manual cell counting confirmed that Setanaxib (GKT137831) attenuates hypoxia-induced pulmonary vascular cell proliferation. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 体内研究(In Vivo) |
During the last half of CCl 4 injections, some mice are treated with Setanaxib (GKT137831) daily. CCl 4 -induced liver fibrosis is more pronounced in SOD1mu compared to WT mice. Liver fibrosis in both SOD1mu and WT mice is attenuated by Setanaxib (GKT137831) treatment. The increased hepatic α-SMA expression is markedly decreased in SOD1mu mice treated with Setanaxib (GKT137831), to a level similar to that of WT mice given the NOX1/4 inhibitor. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Powder -20°C 3 years；4°C 2 years
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| ClinicalTrial |
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| 参考文献 |
[1]. Aoyama T, et al. Nicotinamide adenine dinucleotide phosphate oxidase in experimental liver fibrosis: GKT137831 as a novel potential therapeutic agent. Hepatology. 2012 Dec;56(6):2316-27.[2]. Green DE, et al. The Nox4 inhibitor GKT137831 attenuates hypoxia-induced pulmonary vascular cell proliferation. Am J Respir Cell Mol Biol. 2012 Nov;47(5):718-26.
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| 溶解度数据 |
In Vitro: DMSO : 125 mg/mL (316.58 mM; Need ultrasonic)配制储备液
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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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