Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TAK-418 是一种选择性、口服活性 LSD1/KDM1A 酶抑制剂,IC50 为 2.9 nM。TAK-418 能解锁异常表观遗传机制,改善神经发育障碍模型中的自闭症症状。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 2,660 | 现货 | ||
5 mg | ¥ 5,820 | 现货 | ||
10 mg | ¥ 7,860 | 现货 | ||
25 mg | ¥ 11,600 | 现货 | ||
50 mg | ¥ 15,700 | 现货 | ||
100 mg | ¥ 21,200 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 5,920 | 现货 |
产品描述 | TAK-418 is a selective and orally active inhibitor of LSD1/KDM1A enzyme with an IC50 of 2.9 nM. TAK-418 unlocks abnormal epigenetic mechanisms and improves autism symptoms in models of neurodevelopmental disorders. |
靶点活性 | LSD1/KDM1A:2.9 nM |
体内活性 |
TAK-418 (1 mg/kg; oral; once daily for 14 days) improves certain autism spectrum disorder (ASD)-like behaviors in rodents that model neurodevelopmental disorders.[1] TAK-418 increases H3K4me1/2/3 and H3K9me2 levels of the Ucp2 gene and induces Ucp2 mRNA expression in primary cultured rat neurons. TAK-418 also increases H3K4me1/2/3 of the Bdnf gene. TAK-418 avoids steric interference of GFI1B in the binding pocket by generating a tightly formylated adduct form of coenzyme flavin adenine dinucleotide (FAD). TAK-418 exhibits favorable pharmacokinetic profiles in rodents and inhibits LSD1 enzymatic activity in the brain without causing hematological toxicity in rodents.[1] A single administration of 1 or 3 mg/kg of TAK-418 increases H3K4me2 levels of the Ucp2 gene in the mouse brain.[1] TAK-418 can improve neurological problems at cellular, molecular, gene expression, functional, and functional levels in the KS mouse model (Kmt2d+/βGeo mice).[2] |
分子量 | 356.91 |
分子式 | C17H25ClN2O2S |
CAS No. | 1818252-53-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 49.5 mg/mL (138.7 mM), Sonication and heating to 60℃ are recommended.
H2O: 15.0 mg/mL (42.0 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O | 1 mM | 2.8018 mL | 14.0091 mL | 28.0183 mL | 70.0457 mL |
5 mM | 0.5604 mL | 2.8018 mL | 5.6037 mL | 14.0091 mL | |
10 mM | 0.2802 mL | 1.4009 mL | 2.8018 mL | 7.0046 mL | |
20 mM | 0.1401 mL | 0.7005 mL | 1.4009 mL | 3.5023 mL | |
DMSO | 50 mM | 0.056 mL | 0.2802 mL | 0.5604 mL | 1.4009 mL |
100 mM | 0.028 mL | 0.1401 mL | 0.2802 mL | 0.7005 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
TAK-418 1818252-53-7 Chromatin/Epigenetic Histone Demethylase TAK 418 TAK418 Inhibitor inhibitor inhibit