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首页-小分子抑制剂&激动剂-Others-Pyruvate Kinase-AG-946
AG-946

Chemical Structure : AG-946

CAS No.: 2283422-04-6

AG-946 (Tebapivat, AG946)

货号: PC-21605Not For Human Use, Lab Use Only.

AG-946 (Tebapivat, AG946) is a potent, allosteric activator of wild-type and mutant RBC-specific form of pyruvate kinase (PKR) with AC50 of 5 nM for human wild-type PK, 4.3 nM and 6.9 nM for mutated K410E and R510Q PK proteins, resepctively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    AG-946 (Tebapivat, AG946) is a potent, allosteric activator of wild-type and mutant RBC-specific form of pyruvate kinase (PKR) with AC50 of 5 nM for human wild-type PK, 4.3 nM and 6.9 nM for mutated K410E and R510Q PK proteins, resepctively.
    AG-946 activates both WT PKR and a panel of prototypically unstable PKR mutants.
    AG-946 stabilizes PKR R510Q, an unstable mutant PKR enzyme, and preserves its catalytic activity under increasingly denaturing conditions.
    AG-946 demonstrated good activity in cell-based assays using purified RBCs, with an average AC50 for PKR activation of 35 nM and an average maximum percent PKR activation of 197%.
    AG-946 represents a new investigational PK activator with potential for low projected human drug load and long pharmacodynamic duration of action, suitable for clinical development in a broad range of hemolytic anemias and diseases characterized by dyserythropoiesis.

    物理化学性质&存储条件

    分子量 392.44
    分子式 C18H16N8OS
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    2-((1H-pyrazol-3-yl)methyl)-6-((6-aminopyridin-2-yl)methyl)-4-methyl-4,6-dihydro-5H-thiazolo[5',4':4,5]pyrrolo[2,3-d]pyridazin-5-one

    参考文献

    1. Liu T, et al. ChemMedChem. 2023 Dec 18:e202300559.

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