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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1485.77

C₇₄H₉₆N₁₄O₁₅S₂

174688-78-9

Cys-Lys-Phe-Phe-{d-Trp}-Phe-Thr-Phe-Thr-Ser-Cys (Modifications: Cyclic Cys1-Cys11, X=4-[[(1-methylethyl)amino]methyl]-Phe)

CKFF-{d-Trp}-XTFTSC (Modifications: Cyclic Cys1-Cys11, X=4-[[(1-methylethyl)amino]methyl]-Phe)

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. L Chen, et al. Structural basis for the binding specificity of a SSTR1-selective analog of somatostatin. Biochem Biophys Res Commun. 1999 May 19;258(3):689-94.  [Content Brief]

  [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.  [Content Brief]

  [3]. Per Nilsson, et al. Somatostatin receptor subtypes 1 and 4 redundantly regulate neprilysin, the major amyloid β-degrading enzyme, in brain.