| Identification | Back Directory | [Name]
CH-275 | [CAS]
174688-78-9 | [Synonyms]
CH-275
CYS-LYS-PHE-PHE-D-TRP-IAMP-THR-PHE-THR-SER-CYS
[DES-ALA1, DES-GLY2, DES-ASN5, D-TRP8, IAMP9]SOMATOSTATIN-14
Cys-Lys-Phe-Phe-D-Trp-IAMp-Thr-Phe-Thr-Ser-Cys (Disulfide bridge Cys3-Cys14) | [Molecular Formula]
C74H96N14O15S2 | [MDL Number]
MFCD02264518 | [MOL File]
174688-78-9.mol | [Molecular Weight]
1485.79 |
| Chemical Properties | Back Directory | [Boiling point ]
1732.9±65.0 °C(Predicted) | [density ]
1.235±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Powder | [pka]
2.93±0.70(Predicted) | [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) |
| Hazard Information | Back Directory | [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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| Company Name: |
BOC Sciences
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1-631-485-4226; 16314854226 |
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https://www.bocsci.com |
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