ASK1-IN-1
目录号: PL08711 纯度: ≥99%
CAS No. :2411382-24-4
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中文名称
ASK1-IN-1
英文名称
ASK1-IN-1
英文别名
ASK1-IN-1;N-(6-(4-Isopropyl-4H-1,2,4-triazol-3-yl)pyridin-2-yl)-3-methoxy-1-(pyrazin-2-yl)-1H-pyrazole-4-carboxamide;3-methoxy-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]-1-pyrazin-2-ylpyrazole-4-carboxamide;3-methoxy-N-{6-[4-(propan-2-yl)-4H-1,2,4-triazol-3-yl]pyridin-2-yl}-1-(pyrazin-2-yl)-1H-pyrazole-4-carboxamide;BDBM50538437;E73469;RFG
Cas No.
2411382-24-4
分子式
C19H19N9O2
分子量
405.41
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
ASK1-IN-1 是一种中枢神经系统渗透剂凋亡信号调节激酶 1 (ASK1) 抑制剂,具有良好的效价 (细胞 IC50=138 nM; Biochemical IC50=21 nM)。
生物活性
ASK1-IN-1 is a CNS-penetrant ASK1 (apoptosis signal-regulating kinase 1) inhibitor, with good potency (cell IC 50 =138 nM; Biochemical IC 50 =21 nM).
性状
Solid
IC50 & Target[1][2]
IC50: 138/21 nM (ASK1 in cell and Biochemical assays, respectively)
体外研究(In Vitro)
ASK1-IN-1 (compound 21) has superior CYP inhibition profile and it is also inactive in a hERG assay. ASK1-IN-1 is selected for a kinase selectivity profile against a panel of 468 kinases and it is found to be moderately selective. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
ASK1-IN-1 (10 mg/kg; p.o.) covers the cellular IC 50 /IC 70 /IC 90 at trough in the brain for 12 hours of 50/115/435 mg/kg respectively. ASK1-IN-1 has good biochemical and cellular potency, low clearance and good brain penetration in rodents. has not independently confirmed the accuracy of these methods. They are for reference only.
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]. Xin Z, et al. Discovery of CNS-Penetrant Apoptosis Signal-Regulating Kinase 1 (ASK1) Inhibitors. ACS Med Chem Lett. 2020;11(4):485-490. Published 2020 Feb 12.
溶解度数据
In Vitro: DMF : 4 mg/mL (9.87 mM; Need ultrasonic)DMSO : < 1 mg/mL (insoluble or slightly soluble)Ethanol : < 1 mg/mL (ultrasonic) (insoluble)
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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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