CH 275
Based on 1 publication(s) in Google Scholar
CH 275 is a peptidic somatostatin analog that acts as an agonist of SST1 (IC50 = 30.9 nM, Ki = 52 nM). The IC50 values of CH 275 for sst3, sst4, sst2, and sst5 are 345 nM, >1 μM, >10 μM, and >10 μM, respectively. CH 275 binds to SSTR1 via the IAmp9-Asp137 ion pair interaction and the hydrophobic interaction between the isopropyl group of IAmp9 and Leu107, and reduces the extracellular acidification rate. CH 275 induces weak sst1 internalization, exerts immunosuppressive effects on macrophages, and decreases macrophage viability, MCP-1 expression/secretion, and IL-8 secretion, but does not alter proMMP-9 secretion or IL-8 mRNA levels. CH 275 reduces hippocampal β-amyloid levels and alleviates plaque pathology without inducing hippocampal microglial activation. CH 275 is used in research on Alzheimer's disease, Parkinson's disease, and depression.
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- 純度 : 99.52%
- CAS 番号: 174688-78-9
- 分子式: C74H96N14O15S2
- 分子量:1485.77
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保管条件:
Sealed storage, away from moisture and light.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 CH 275
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生物活性
製品説明
IC50 & Target
[1]|
SSTR1 |
体外実験
CH 275 (1 μM; 24 h) induces weak internalization of sst1 receptors in LPS-activated human macrophages differentiated from PBMC-derived monocytes after 24 h of treatment[1].
CH-275 (1 μM; 24 h) does not affect proMMP-9 secretion from LPS-activated human macrophages differentiated from PBMC-derived monocytes[1].
CH 275 (1 μM; 24 h) reduces IL-8 secretion without affecting IL-8 mRNA levels in LPS-activated human macrophages differentiated from PBMC-derived monocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS-activated human macrophages differentiated from PBMC-derived monocytes
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Concentration:1 μM
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Incubation Time:24 h
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Result:Decreased basal absorbance (a measure of viable cell number/metabolic activity) by 78%.
Showed viability-reducing effect that was completely reversed by co-application of the sst1-selective antagonist SRA-880.
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Cell Line:LPS-activated human macrophages differentiated from PBMC-derived monocytes
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Concentration:1 μM
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Incubation Time:24 h
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Result:Induced weak punctate sst1 immunoreactivity inside cells in addition to surface-localized receptor, indicating a weak level of sst1 receptor internalization.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (AppNL-G-F knock-in; 2 months of age at start of administration)[4]
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Dosage:56 µM (infusate concentration); 2 µM (measured total hippocampal concentration); 100 nM (targeted interstitial fluid concentration)
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Administration:i.c.v. (brain infusion cannula connected to osmotic pump); continuous; 4 months; flow rate 0.11 µl/h
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Result:Robustly increased neprilysin expression in the ipsilateral hippocampus compared to the contralateral side.
Reduced Aβ levels on the ipsilateral side.
Showed a trend toward improved memory performance in the Y-maze.
Significantly reduced anxiety level in the open field test.
Showed no significant difference in microglial activation compared to PBS-injected mice in either the ipsilateral or contralateral hippocampus via Iba1 staining.
Caused no toxic side effects.
化学情報
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CAS 番号 174688-78-9
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性状 Solid
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分子量 1485.77
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分子式 C74H96N14O15S2
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Color White to off-white
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配列
Cys-Lys-Phe-Phe-{d-Trp}-Phe-Thr-Phe-Thr-Ser-Cys (Modifications: Cyclic Cys1-Cys11, X=4-[[(1-methylethyl)amino]methyl]-Phe)
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シーケンスの短縮
CKFF-{d-Trp}-XTFTSC (Modifications: Cyclic Cys1-Cys11, X=4-[[(1-methylethyl)amino]methyl]-Phe)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture and light
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (67.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (33.65 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
[2]. Chen L, et al. Structural basis for the binding specificity of a SSTR1-selective analog of somatostatin. Biochemical and biophysical research communications. 1999 May 19;258(3):689-94. [Content Brief]
[5]. Rivier JE, et al. Potent somatostatin undecapeptide agonists selective for somatostatin receptor 1 (sst1). J Med Chem. 2001 Jun 21;44(13):2238-46. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 0.6731 mL | 3.3653 mL | 6.7305 mL | 16.8263 mL |
| 5 mM | 0.1346 mL | 0.6731 mL | 1.3461 mL | 3.3653 mL | |
| 10 mM | 0.0673 mL | 0.3365 mL | 0.6731 mL | 1.6826 mL | |
| 15 mM | 0.0449 mL | 0.2244 mL | 0.4487 mL | 1.1218 mL | |
| 20 mM | 0.0337 mL | 0.1683 mL | 0.3365 mL | 0.8413 mL | |
| 25 mM | 0.0269 mL | 0.1346 mL | 0.2692 mL | 0.6731 mL | |
| 30 mM | 0.0224 mL | 0.1122 mL | 0.2244 mL | 0.5609 mL | |
| DMSO | 40 mM | 0.0168 mL | 0.0841 mL | 0.1683 mL | 0.4207 mL |
| 50 mM | 0.0135 mL | 0.0673 mL | 0.1346 mL | 0.3365 mL | |
| 60 mM | 0.0112 mL | 0.0561 mL | 0.1122 mL | 0.2804 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
CH 275 関連分類
HY-P1206 関連分類
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