| 公司名称： |
上海波以尔化工有限公司 |
| 联系电话： |
Mr Qiu 86-21-50182298(Domestic Market)Miss Xu 86-21-50180596(Abroad Market) |
| 产品介绍： |
中文名称:N-(6-氟-1H-吲唑-5-基)-2-甲基-6-氧代-4-[4-(三氟甲基)苯基]-1,4,5,6-四氢-3-吡啶甲酰胺
英文名称:N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-4-(trifluoromethyl)phenyl-1,4,5,6-tetrahydro-3-pyridinecarboxamide
CAS:864082-47-3
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| 公司名称： |
武汉易泰科技有限公司上海分公司 |
| 联系电话： |
86-21-50328103 * 801、802、803、804 Mobile:18930552037 |
| 产品介绍： |
中文名称:N-(6-氟-1H-吲唑-5-基)-2-甲基-6-氧代-4-[4-(三氟甲基)苯基]-1,4,5,6-四氢-3-吡啶甲酰胺
英文名称:N-(6-Fluoro-1H-indazol-5-yl)-2-Methyl-6-oxo-4-[4-(trifluoroMethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxaMide
CAS:864082-47-3
纯度：99% HPLC 包装信息：1Mg ; 5Mg;10Mg ;100Mg;250Mg ;500Mg ;1g;2.5g ;5g ;10g |
| 公司名称： |
上海佰世凯化学科技有限公司 |
| 联系电话： |
+86(0)21-20908456 |
| 产品介绍： |
英文名称:GSK 429286 A
CAS:864082-47-3
备注：C14617 |
| 公司名称： |
石家庄斯迪亚诺精细化工有限公司 |
| 联系电话： |
+86-311-89250318 |
| 产品介绍： |
中文名称:N-(6-氟-1H-吲唑-5-基)-2-甲基-6-氧代-4-[4-(三氟甲基)苯基]-1,4,5,6-四氢-3-吡啶甲酰胺
英文名称:N-(6-Fluoro-1H-indazol-5-yl)-2-Methyl-6-oxo-4-[4-(trifluoroMethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxaMide
CAS:864082-47-3
纯度：98% |
| 公司名称： |
凯方医药科技（上海）有限公司 |
| 联系电话： |
021-67220633 & 021-37212706 |
| 产品介绍： |
英文名称:N-(6-Fluoro-1H-indazol-5-yl)-2-Methyl-6-oxo-4-[4-(trifluoroMethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxaMide
CAS:864082-47-3
纯度：99% 包装信息：5KG;1KG |
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| 中文名称: | GSK429286A | | 中文同义词: | N-(6-氟-1H-吲唑-5-基)-2-甲基-6-氧代-4-[4-(三氟甲基)苯基]-1,4,5,6-四氢-3-吡啶甲酰胺 | | 英文名称: | GSK429286A | | 英文同义词: | N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide;RHO-15(GSK429286A);GSK 429286 A;RHO-15;N-(6-fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-(4-(trifluoromethyl)phenyl)-1,4,5,6-tetrahydropyridine-3-carboxamide;GSK 429286 A
N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide;N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide GSK 429286 A;N-(6-Fluoro-1H-indazol-5-yl)-1,4,5,6-tetrahydro-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-3-pyridinecarboxamide | | CAS号: | 864082-47-3 | | 分子式: | C21H16F4N4O2 | | 分子量: | 432.37 | | EINECS号: | | | 相关类别: | |
| 生物活性 | GSK429286A是一种选择性的ROCK1和ROCK2抑制剂，IC50分别为14 nM和63 nM。 | | 体外研究 | GSK429286A slightly inhibits RSK and p70S6K with IC50 of 0.78 μM and 1.94 μM, respectively. GSK429286A significantly inhibits rat aortic ring dilation with IC50 of 190 nM. GSK429286A at 1 μM reduces ROCK2 activity over 20-fold, under conditions in which the only other kinase tested that is significantly inhibited is MSK1 whose activity is reduced ~5-fold. GSK429286A is a more selective ROCK2 inhibitor than the widely utilized ROCK inhibitor Y-27632 as assessed on kinase-specificity panel, and does not significantly inhibit LRRK2 even at doses as high as 30 μM (500-fold higher than IC50 of inhibition of ROCK2). Like GSK269962A but not sunitinib, GSK429286A treatment at 10 μM ablates basal or G14V-Rho mutant induced phosphorylation of MYPT at Thr850 in HEK-293 cells to a similar extent as H-1152 and Y-27632, consistent with ROCK mediating this phosphorylation, whereas GSK429286A does not inhibit ERM protein phosphorylation either in the presence or absence of G14V-Rho. | | 体内研究 | GSK429286A has 61% oral bioavailability in male Sprague-Dawley rats. Oral administration of GSK429286A at single doses of 3-30 mg/kg dramatically reduces mean arterial pressure in the spontaneously hypertensive rats (SHRs) in a dose-dependent manner, with a maximum decrease of 50 mmHg after approximately 2 hours treatment at dose of 30 mg/kg. | | 特征 | More selective than Y-27632. |
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