UGT8 inhibitor 19

Chemical Structure : UGT8 inhibitor 19

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货号: PC-21184Not For Human Use, Lab Use Only.

UGT8 inhibitor 19 is a highly potent, selective and orally active ceramide galactosyltransferase enzyme UGT8 inhibitor with IC50 of 0.2 nM.

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生物&药学活性

UGT8 inhibitor 19 is a highly potent, selective and orally active ceramide galactosyltransferase enzyme UGT8 inhibitor with IC50 of 0.2 nM.
UGT8 inhibitor 19 is selective for inhibition of UGT8 compared to other UGT enzymes (IC50 > 10 μM for UGT1A1, UGT1A6, UGT2B7, UGT2B15, and UGT2B17) and a Cerep panel of around 60 kinases.
UGT8 inhibitor 19 demonstrated dose dependent inhibition of incorporation of 13C-Gal into GalCer and SFT in adult mice kidney with an estimated ED50 of 1 mg/kg for inhibition of both SFT and GalCer.
UGT8 inhibitor 19 showed efficacy in the in vivo pharmacodynamic models, indicating the potential to treat metachromatic leukodystrophy (MLD).

物理化学性质&存储条件

分子量	528.47
分子式	C20H22F6N4O4S
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	1-[3-[(Methylamino)carbonyl]-7-(trifluoromethyl)thieno[3,2-b]pyridin-5-yl]-4-piperidinyl N-[(1S)-1-methyl-2-(trifluoromethoxy)ethyl]carbamate

参考文献

1. Sukanthini Thurairatnam, et al. ACS Med Chem Lett. 2020 Jun 16;11(10):2010-2016.