SMS2-IN-3

Names

[ CAS No. ]:
2414240-89-2

[ Name ]:
SMS2-IN-3

Biological Activity

[Description]:

SMS2-IN-3 is a potent and selective SMS2inhibitor (IC50=2.2 nM), significantly reduces the hepatic SM (22:0) levels[1].

[Related Catalog]:

Research Areas >> Cancer
Research Areas >> Infection
Research Areas >> Others
Signaling Pathways >> Others >> Others

[Target]

IC50: 2.2nM (SMS2)[1]


[In Vitro]

SMS2-IN-3 (37) is an excellent sphingomyelin synthase 2 inhibitor (SMS2). SMS2-IN-3 (37) has inhibition (IC50= 2.2 nM) and good selectivity against SMS1[1]. Cell Viability Assay[1] Cell Line: FreeStyle293 cells Concentration: 100mg/kg Incubation Time: 60 min Result: Showed excellent SMS2 inhibition and good selectivity against SMS1 in biological evaluation.

[In Vivo]

SMS2-IN-3 (37) has excellent SMS2 activity and high selectivity against SMS1. SMS2-IN-3 also reduces the level of SM by subcutaneous treatment[1]. Animal Model: KK-Ay/Ta mice[1] Dosage: 100, 200 mg/kg Administration: SMS2-IN-3: s.c. (100, 200 mg/kg); p.o. (100, 200 mg/kg); once or twice per day for 7 days. Result: cmpd Cmax, (μg/mL) Tmax, (h) C24 h, (μg/mL) AUC0-24(μg•h/mL) MRT(h) 37(p.o.) 6.5 0.83 0.007 18 3.0 37(s.c.) 0.70 8.0 0.23 12 9.4

[References]

[1]. Takafumi Yukawa, et al. Discovery of 1,8-naphthyridin-2-one derivative as a potent and selective sphingomyelin synthase 2 inhibitor. Bioorg Med Chem. 2020 Apr 1;28(7):115376.

Chemical & Physical Properties

[ Molecular Formula ]:
C33H39F3N4O6

[ Molecular Weight ]:
644.68

Related Compounds