SPL-410 | SPPL2a inhibitor | Probechem Biochemicals

Chemical Structure : SPL-410

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SPL-410 (SPL410)

货号: PC-73009Not For Human Use, Lab Use Only.

SPL-410 (SPL410) is a highly potent, selective, orally active inhibitor SPPL2a (Signal Peptide Peptidase Like 2a) with IC50 of 9 nM.

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生物&药学活性

SPL-410 (SPL410) is a highly potent, selective, orally active inhibitor SPPL2a (Signal Peptide Peptidase Like 2a) with IC50 of 9 nM.
Both human and mouse SPPL2a was inhibited with high potency (IC50 of 0.004 μM and 0.005 μM) in high content imaging assay (HCA).
SPL-410 is selective against closely related human aspartyl proteases such as SPP (0.65 μM) and γ-secretase (1.3 μM) as well as SPPL2b (0.27 μM in HCA)
SPL-410 inhibited the processing of the endogenous substrate CD74/p8 NTF in IC50 of 0.15 μM in the mouse B cell line A20.
SPL-410 caused accumulation of CD74/p8 NTF (10 mg/kg single p.o. dose) in mice, achieved a higher efficacy than LY-411575.

物理化学性质&存储条件

分子量	500.58
分子式	C24H31F3N2O4S
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	Benzenesulfonamide, N-[(2S,3S)-3-amino-2-hydroxy-3-[4-(trifluoromethoxy)phenyl]propyl]-N-cyclobutyl-4-(1,1-dimethylethyl)-

参考文献

1. Velcicky J, et al. ACS Med Chem Lett. 2019 May 23;10(6):887-892.

SPL-410 (SPL410)

生物&药学活性

物理化学性质&存储条件

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SPL-410 (SPL410)

生物&药学活性

物理化学性质&存储条件

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