Description |
CH 275 is a potent and selective somatostatin receptor 1 (sst1) agonist and display IC50 values of 30.9 nM, 345 nM, >1 μM, >10 μM for human human sst1, sst3, sst4, sst2 and sst5 respectively[1]. CH 275 can be used for the research of Alzheimer’s disease[2].
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Related Catalog |
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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[1].
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In Vivo |
CH275 (osmotic pump administration; 56 μM; two weeks) decreases the level of neprilysin/SRIF in the App knock-in mice[1]. CH275 directly injects into the Lmol layer of 2-month-old AppNL-G-Fmice for four months. AppNL-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[1].
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References |
[1]. J E Rivier, et al. Potent somatostatin undecapeptide agonists selective for somatostatin receptor 1 (sst1). J Med Chem. 2001 Jun 21;44(13):2238-46. [2]. J E Rivier, et al. Potent somatostatin undecapeptide agonists selective for somatostatin receptor 1 (sst1). J Med Chem. 2001 Jun 21;44(13):2238-46.
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