SPL-707 |
Catalog No.GC31854 |
SPL-707은 hSPPL2a에 대한 IC50이 77nM인 경구 활성 선택적 신호 펩티드 펩티다제 유사 2a(SPPL2a) 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2195361-33-0
Sample solution is provided at 25 µL, 10mM.
SPL-707 is a potent, selective and orally available signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 80 nM.
SPL-707 shows 25-fold selectivity over SPP with an IC50 of 3.7 μM and some preference for SPPL2a over SPPL2b with a 3-fold selectivity, comparing IC50 values generated with comparable assay formats for the different proteases[1].
SPL-707 significantly inhibits processing of the SPPL2a substrate CD74/p8 fragment in rodents at doses ≤10 mg/kg b.i.d. po. Oral dosing of SPL-707 for 11 days at ≥10 mg/kg b.i.d. recapitulates the phenotype seen in Sppl2a knockout (ko) and ENU mutant mice (reduced number of specific B cells and myeloid dendritic cells)[1].
[1]. Velcicky J, et al. Discovery of the First Potent, Selective, and Orally Bioavailable Signal Peptide Peptidase-Like 2a (SPPL2a) Inhibitor Displaying Pronounced Immunomodulatory Effects In Vivo. J Med Chem. 2018 Feb 8;61(3):865-880.
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