Chemical Structure : SPL-707
货号: PC-62535Not For Human Use, Lab Use Only.
SPL-707 (SPL707) is the first selective, orally active signal peptide peptidase-like 2a (SPPL2a) inhibitor with IC50 of 77 nM, shows 25-fold selectivity over γ-secretase and SPP.
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SPL-707 (SPL707) is the first selective, orally active signal peptide peptidase-like 2a (SPPL2a) inhibitor with IC50 of 77 nM, shows 25-fold selectivity over γ-secretase and SPP.
SPL-707 significantly inhibits processing of the SPPL2a substrate CD74/p8 fragment in rodents at doses ≤10 mg/kg b.i.d. po., recapitulates the phenotype seen in Sppl2a knockout (ko) and ENU mutant mice after oral dosing of 40 for 11 days at ≥10 mg/kg b.i.d.
分子量 | 505.55 | |
分子式 | C27H28FN5O4 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Velcicky J, et al. J Med Chem. 2018 Feb 8;61(3):865-880.
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