Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
1 mg | 在庫あり | ¥ 53,500 |
5 mg | 在庫あり | ¥ 133,000 |
10 mg | 在庫あり | ¥ 209,500 |
25 mg | 在庫あり | ¥ 429,500 |
50 mg | 在庫あり | ¥ 578,500 |
100 mg | 在庫あり | ¥ 776,000 |
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 156,000 |
説明 | 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. |
ターゲット&IC50 | LSD1/KDM1A:2.9 nM |
In vivo |
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)
You can also refer to dose conversion for different animals. 詳細
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TAK-418 1818252-53-7 Chromatin/Epigenetic Histone Demethylase TAK 418 TAK418 Inhibitor inhibitor inhibit