CH 275

CH 275 is a peptide analog of somatostatin and binds preferably to somatostatin receptor 1 (sst₁) with a K_i of 52 nM^[1]. CH 275 acts as a potent and selective sst₁?agonist (IC₅₀=30.9 nM) and also displays?IC₅₀?values of 345 nM, >1?μM, >10?μM, >10?μM for human sst₃, sst₄, sst₂?and sst₅,?respectively^[2]. CH 275 can be used for the research of alzheimer’s disease^[3]. IC50 & Target:IC50: 30.9 nM; Ki: 52 nM (somatostatin receptor 1)^[1][2]
IC50: 345 nM (somatostatin receptor 3)^[1] In Vitro: CH275 (100 nM) activates neprilysin activity, wheras treatment with cyclo-SRIF can complete this activation in vitro in primary neuron-based cell culture system, a mixture of wildtype hippocampal, cortical and striatal neuron^[3].
In Vivo: CH275 (osmotic pump administration; 56 μM; two weeks) decreases the?level of neprilysin/SRIF in the?App?knock-in mice^[3].
CH275 directly injects into the Lacunosum molecular layer (Lmol) layer of 2-month-old App^NL-G-F mice for four months. App^NL-G-F mice begin to exhibit Aβ plaques at two months of age, but CH275 leads to robustly increased the expression of neprilysin in hippocampus which is paralleled by a clear reduction in Aβ plaque load in the same region, and without causing any toxic side effects^[3].