DDD02049209

Chemical Structure : DDD02049209

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货号: PC-25240Not For Human Use, Lab Use Only.

DDD02049209 is a potent, specific inhibitor of M. tuberculosis lysyl-tRNA synthetase (LysRS) with IC50 of 0.05 uM, inhibits M. tuberculosis phenotypic growth in culture (MIC) with 0.08 uM.

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生物&药学活性

DDD02049209 is a potent, specific inhibitor of M. tuberculosis lysyl-tRNA synthetase (LysRS) with IC50 of 0.05 uM, inhibits M. tuberculosis phenotypic growth in culture (MIC) with 0.08 uM.
DDD02049209 displays exquisite selectivity (>100-fold) over the human counterpart, at both an enzyme (KARS1, IC50 > 100 μM; and cellular level (HepG2 IC50 > 100 μM).
DDD02049209 demonstrates good efficacy, achieving a >3 log10 reduction in colony forming units (CFU) with an ED99 (dose that causes a 2 Log10 reduction in CFU with respect to untreated mice) of 49 and 12 mg/kg respectively in murine models of M. tuberculosis infection, achieved a clear reduction in lung CFU, with a maximum effect of 2.4 log10 reductions and an ED99 of 94 mg/kg.

物理化学性质&存储条件

分子量	328.32
分子式	C14H18F2N4O3
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-amino-6-((1S,7S)-2,2-difluoro-7-hydroxycycloheptyl)-4-methoxy-6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidin-5-one

参考文献

1. Green SR, et al. Nat Commun. 2022 Oct 11;13(1):5992.

DDD02049209

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物理化学性质&存储条件

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DDD02049209

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