CH-275
CH-275 Basic information
- 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
- 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
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 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].
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].
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] Per?Nilsson,?et al. Somatostatin receptor subtypes 1 and 4 redundantly regulate neprilysin, the major amyloid β-degrading enzyme, in brain.
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