KARI-201 is a multifunctional small molecule that demonstrates dual activity as a highly selective inhibitor of acid sphingomyelinase (ASM) and an agonist of the ghrelin receptor. It operates as a competitive inhibitor by binding directly to the active site of ASM. Studies reveal that the incorporation of KARI-201 into ASM decreases in a concentration-dependent manner with sphingomyelin, resulting in KM values of 332.5, 433.9, and 572.6 μM at KARI-201 concentrations of 1, 10, and 100 μM, respectively. In preclinical models, KARI-201 has shown efficacy in reducing amyloid pathology and reversing cognitive deficits in APP/PS1 mice. Additionally, it enhances autophagy degradation by promoting lysosomal biogenesis in neuronal cells. As a ghrelin receptor agonist, KARI-201 also supports hippocampal neurogenesis and improves synaptic plasticity, making it a promising therapeutic candidate for neurodegenerative conditions.
Cat.No
DC70536
Name
KARI 201
Chemical Properties
CAS
2376132-22-6
Formula
C14H28N4O2
MW
284.404
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
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