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| Product Name: | CH-275 | | Synonyms: | 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: | 174688-78-9 | | MF: | C74H96N14O15S2 | | MW: | 1485.79 | | EINECS: | | | Product Categories: | | | Mol File: | 174688-78-9.mol |  |
| | CH-275 Chemical Properties |
| Boiling point | 1732.9±65.0 °C(Predicted) | | density | 1.235±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | pka | 2.93±0.70(Predicted) | | form | Powder | | color | White to off-white | | Water Solubility | Soluble to 0.30 mg/ml in water | | Sequence | Cys-Lys-Phe-Phe-{d-Trp}-Phe-Thr-Phe-Thr-Ser-Cys (Modifications: Cyclic Cys1-Cys11, X=4-[[(1-methylethyl)amino]methyl]-Phe) |
| | CH-275 Usage And Synthesis |
| Uses | 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 sst1agonist (IC50=30.9 nM) and also displaysIC50values of 345 nM, >1μM, >10μM, >10μM for human sst3, sst4, sst2and sst5,respectively[2]. CH 275 can be used for the research of alzheimer’s disease[3]. | | in vivo | CH275 (osmotic pump administration; 56 μM; two weeks) decreases thelevel of neprilysin/SRIF in theAppknock-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]. | | IC 50 | SSTR1 | | References | [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. DOI:10.1006/bbrc.1999.0699
[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. DOI:10.1021/jm010037+
[3] PerNilsson,et al. Somatostatin receptor subtypes 1 and 4 redundantly regulate neprilysin, the major amyloid β-degrading enzyme, in brain. |
| | CH-275 Preparation Products And Raw materials |
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