生长抑素肽类似物
中文名称 | 生长抑素肽类似物 |
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中文同义词 | 生长抑素肽类似物 |
英文名称 | CH-275 |
英文同义词 | CYS-LYS-PHE-PHE-D-TRP-IAMP-THR-PHE-THR-SER-CYS;[DES-ALA1, DES-GLY2, DES-ASN5, D-TRP8, IAMP9]SOMATOSTATIN-14;CH-275;Cys-Lys-Phe-Phe-D-Trp-IAMp-Thr-Phe-Thr-Ser-Cys (Disulfide bridge Cys3-Cys14);L-Cysteine, L-cysteinyl-L-lysyl-L-phenylalanyl-L-phenylalanyl-D-tryptophyl-4-[[(1-methylethyl)amino]methyl]-L-phenylalanyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-, cyclic (1→11)-disulfide;CKFF-{d-Trp}-XTFTSC (Modifications: Cyclic Cys1-Cys11, X=4-[[(1-methylethyl)amino]methyl]-Phe) |
CAS号 | 174688-78-9 |
分子式 | C74H96N14O15S2 |
分子量 | 1485.79 |
EINECS号 | |
相关类别 | |
Mol文件 | 174688-78-9.mol |
结构式 | ![]() |
生长抑素肽类似物 性质
沸点 | 1732.9±65.0 °C(Predicted) |
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密度 | 1.235±0.06 g/cm3(Predicted) |
储存条件 | Store at -20°C |
酸度系数(pKa) | 2.93±0.70(Predicted) |
形态 | 粉末 |
颜色 | 白色至米白色 |
水溶解性 | Soluble to 0.30 mg/ml in water |
IC50: 30.9 nM; Ki: 52 nM (somatostatin receptor 1)IC50: 345 nM (somatostatin receptor 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.
CH275 (osmotic pump administration; 56 μM; two weeks) decreases the level of neprilysin/SRIF in the App knock-in mice.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.