For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | P000175 |
| CAS Number | 174688-78-9 |
| Synonyms | (4R,7S,10S,13S,16S,19S,22R,25S,28S,31S,34R)-34-amino-31-(4-aminobutyl)-13,25,28-tribenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30,33-decaoxo-19-[[4-[(propan-2-ylamino)methyl]phenyl]methyl]-1,2-dithia-5,8,11,14,17,20,23,26,29,32-decazacyclopentatriacontane-4-carboxylic acid |
| Molecular Formula | C74H96N14O15S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C74H96N14O15S2/c1-42(2)77-37-49-29-27-48(28-30-49)35-57-69(97)87-62(43(3)90)72(100)84-58(34-47-22-12-7-13-23-47)70(98)88-63(44(4)91)73(101)85-60(39-89)71(99)86-61(74(102)103)41-105-104-40-52(76)64(92)79-54(26-16-17-31-75)65(93)80-55(32-45-18-8-5-9-19-45)66(94)81-56(33-46-20-10-6-11-21-46)67(95)83-59(68(96)82-57)36-50-38-78-53-25-15-14-24-51(50)53/h5-15,18-25,27-30,38,42-44,52,54-63,77-78,89-91H,16-17,26,31-37,39-41,75-76H2,1-4H3,(H,79,92)(H,80,93)(H,81,94)(H,82,96)(H,83,95)(H,84,100)(H,85,101)(H,86,99)(H,87,97)(H,88,98)(H,102,103)/t43-,44-,52+,54+,55+,56+,57+,58+,59-,60+,61+,62+,63+/m1/s1 |
| InChIKey | SYHQUPOPQRNSKD-SKMHOITNSA-N |
| SMILES | CC(C)NCC1=CC=C(C=C1)CC2C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC3=CNC4=CC=CC=C43)CC5=CC=CC=C5)CC6=CC=CC=C6)CCCCN)N)C(=O)O)CO)C(C)O)CC7=CC=CC=C7)C(C)O |
| Reference | [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. |
