化合物TAK-418 T39252

Product Introduction
Bioactivity


英文名: TAK-418

描述: 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。

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]

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

溶解度: DMSO : 49.5 mg/mL (138.7 mM)
H2O : 15.0 mg/mL (42.0 mM)


关键字: TAK-418 | TAK 418 | TAK418

相关产品: KDM5-IN-1 | LSD1-UM-109 | LSD1-IN-5 | Methylstat | S2101 | Ryuvidine | KF 13218 | Pulrodemstat benzenesulfonate | JMJD7-IN-1 | GSK2879552 2HCl (1401966-69-5(free base))

相关库: Drug Repurposing Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Covalent Inhibitor Library | Histone Modification Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途