CH 275

发表于由

CH 275;

CH 275 是一种生长抑素的肽类似物，可以与生长抑素受体1 (sst1) 结合 (Ki=52 nM)。CH 275 是一种有效的选择性 sst1 激动剂 (IC50=30.9 nM)，刺激 sst3，sst4，sst2 和 sst5 的 IC50 值 分别为 345 nM，>1 μM，>10 μM 和 >10 μM。CH 275 可用于阿尔茨海默病的研究。

CH 275amp;;

CH 275 Chemical Structure

CAS No. : 174688-78-9

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生物活性

CH 275 is a peptide analog of somatostatin and binds preferably to somatostatin receptor 1 (sst1) with a Ki 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]
体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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 AppNL-G-F mice 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[3].

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

1485.77

Formula

C74H96N14O15S2
CAS 号

174688-78-9
Sequence Shortening

CKFFWXTFTSC (Modifications: Cyclic Cys1-Cys11, X=4-[[(1-methylethyl)amino]methyl]-Phe)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

  • [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.

    [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.

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