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MRT67307 HCl (1190378-57-4 free base)

MRT67307 HCl (1190378-57-4 free base)

产品编号 T23028   CAS T23028
别名: MRT67307 HCl

MRT67307 is an inhibitor for TBK1, IKKε , MARK1-4 and NUAK1 with IC50 value of 19, 160, 27-52 and 230nM , respectively [1]. It is an inhibitor for ULK1and ULK2 with IC50 value of 45 and 38nM, respectively [2]. Also, it is a salt inducible kinase (SIK) inhibitor with IC50 value of 250, 67 and 430nM for SIK1, SIK2 and SIK3, respectively.<br /<SIKs prevent the formation of regulatory macrophages and their inhibition induces increasing in some markers of regulatory macrophages, such as IL-10 and other anti-inflammatory molecules. IKKε and TBK-1 mediate the phosphorylation of interferon regulatory factor 3 (IRF3). MARK1 is a Serine/threonine-protein kinase.<br /<In macrophages, MRT67307 prevented the production of IFNβ and the phosphorylation of IRF3 without suppressing the activation of NF-κB, which showed that MRT67307 blocked the induction of Pellino 1 through inhibiting TBK1/IKKε kinase activity [1] [3]. Also, MRT67307 completely blocked the TBK1- or IKKε-induced decrease in the mobility of Pellino 1 [3]. Exposed macrophages to MRT67307 increased the levels of the anti-inflammatory cytokines IL-1ra and IL-10 and decreased the levels of proinflammatory cytokines (such as IL-6, IL-12, and TNF) in response to bacterial lipopolysaccharide (LPS) [4].<br /<<em< 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 MRT 67307 dihydrochloride 的水溶性和稳定性通常比游离态更好。

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MRT67307 HCl (1190378-57-4 free base) Chemical Structure
MRT67307 HCl (1190378-57-4 free base), CAS T23028
规格 价格/CNY 货期 数量
5 mg ¥ 726 待询
10 mg ¥ 1,266 待询
50 mg ¥ 3,183 待询
1 mL * 10 mM (in DMSO) ¥ 753 待询

MRT67307 HCl (1190378-57-4 free base) 的其他形式现货产品:

MRT67307 MRT 67307 dihydrochloride MRT67307 HCl (1190378-57-4(free base))
其他形式的 MRT67307 HCl (1190378-57-4 free base):
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
产品目录号及名称: MRT67307 HCl (1190378-57-4 free base) (T23028)
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生物活性
化学信息
存储 & 溶解度
产品描述 MRT67307 is an inhibitor for TBK1, IKKε , MARK1-4 and NUAK1 with IC50 value of 19, 160, 27-52 and 230nM , respectively [1]. It is an inhibitor for ULK1and ULK2 with IC50 value of 45 and 38nM, respectively [2]. Also, it is a salt inducible kinase (SIK) inhibitor with IC50 value of 250, 67 and 430nM for SIK1, SIK2 and SIK3, respectively.<br />SIKs prevent the formation of regulatory macrophages and their inhibition induces increasing in some markers of regulatory macrophages, such as IL-10 and other anti-inflammatory molecules. IKKε and TBK-1 mediate the phosphorylation of interferon regulatory factor 3 (IRF3). MARK1 is a Serine/threonine-protein kinase.<br />In macrophages, MRT67307 prevented the production of IFNβ and the phosphorylation of IRF3 without suppressing the activation of NF-κB, which showed that MRT67307 blocked the induction of Pellino 1 through inhibiting TBK1/IKKε kinase activity [1] [3]. Also, MRT67307 completely blocked the TBK1- or IKKε-induced decrease in the mobility of Pellino 1 [3]. Exposed macrophages to MRT67307 increased the levels of the anti-inflammatory cytokines IL-1ra and IL-10 and decreased the levels of proinflammatory cytokines (such as IL-6, IL-12, and TNF) in response to bacterial lipopolysaccharide (LPS) [4].<br /><em>
别名 MRT67307 HCl
分子量 N/A
分子式 C26H36N6O2· xHCl
CAS No. T23028

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: > 52.5 mg/mL, Heating is recommended.

Ethanol: ≥30.67 mg/mL

DMSO: ≥23.25 mg/mL

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

MRT67307 HCl (1190378-57-4 free base) T23028 Others 1190378-57-4 free base MRT67307 HCl MRT-67307 HCl (1190378-57-4 free base) MRT67307 HCl (1190378 57 4 free base) 1190378-57-4 MRT67307 HCl (1190378574 free base) Inhibitor inhibitor inhibit

 

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