CH 275

CH 275 is a peptide analog of somatostatin and binds preferably to somatostatin receptor 1 (sst1) with a Ki of 52 nM. 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. CH 275 can be used for the research of alzheimer’s disease.

Product information

CAS Number: 174688-78-9

Molecular Weight: 1471.79

Formula: C74H98N14O14S2

Chemical Name: (4R,7R,10R,13S,16R,19R,22S,25S,28S,31R,34R)-34-amino-31-(4-aminobutyl)-13,25,28-tribenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-[(1H-indol-3-yl)methyl]-9,12,15,18,21,24,27,30,33-nonaoxo-19-[(4-{[(propan-2-yl)amino]methyl}phenyl)methyl]-1,2-dithia-5,8,11,14,17,20,23,26,29,32-decaazacyclopentatriacontane-4-carboxylic acid

Smiles: CC(C)NCC1=CC=C(C[C@H]2NC(=O)[C@H](CC3=CNC4=CC=CC=C34)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@H](NC[C@H](CO)NC(=O)[C@H](NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](NC2=O)[C@@H](C)O)[C@@H](C)O)C(O)=O)C=C1

InChiKey: LFOPEPKKBBIGHF-RXUBGYFDSA-N

InChi: InChI=1S/C74H98N14O14S2/c1-43(2)77-37-50-29-27-49(28-30-50)35-59-70(97)88-64(45(4)91)73(100)86-60(34-48-22-12-7-13-23-48)71(98)87-63(44(3)90)72(99)80-52(40-89)39-79-62(74(101)102)42-104-103-41-54(76)65(92)81-56(26-16-17-31-75)66(93)82-57(32-46-18-8-5-9-19-46)67(94)83-58(33-47-20-10-6-11-21-47)68(95)85-61(69(96)84-59)36-51-38-78-55-25-15-14-24-53(51)55/h5-15,18-25,27-30,38,43-45,52,54,56-64,77-79,89-91H,16-17,26,31-37,39-42,75-76H2,1-4H3,(H,80,99)(H,81,92)(H,82,93)(H,83,94)(H,84,96)(H,85,95)(H,86,100)(H,87,98)(H,88,97)(H,101,102)/t44-,45-,52-,54+,56-,57+,58+,59-,60+,61+,62+,63-,64-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

In Vivo:

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 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.

Products are for research use only. Not for human use.