CYN 154806 TFA
| 中文名称 | CYN 154806 TFA |
|---|---|
| 中文同义词 | 环状八肽AC-PHE-CYS-TYR-TRP-LYS-THR-CYS-TYR-NH2 |
| 英文名称 | CYN 154806 TFA |
| 英文同义词 | CYN 154806 TFA |
| CAS号 | |
| 分子式 | C??H??F?N??O??S? |
| 分子量 | 0 |
| EINECS号 | |
| 相关类别 | 目录多肽 |
| Mol文件 | Mol File |
| 结构式 |
CYN 154806 TFA 性质
| 序列 | Ac-Phe-Cys-Tyr-Trp-Lys-Thr-Cys-Tyr-NH2?(Disulfide?bridge:?Cys2-Cys7) |
|---|
CYN 154806 TFA 是一种环状八肽，是一种强效的，选择性生长抑素 sst2 受体的拮抗剂，其对人重组 sst2、sst1、sst3、sst4 和 sst5 受体的 pIC50 值分别为 8.58、5.41、6.07、5.76 和 6.48。
纯度(HPLC) ≥98.0%
醋酸根含量≤12.0%
水分含量≤8.0%
肽含量≥80.0%
内毒素≤50EU/mg
氨基酸组成分析≤±10%
Somatostatin Receptor
CYN 154806 TFA inhibits SRIF-induced increases in extracellular acidification (EAR) in CHO-K1 cells expressing human sst2 receptors (pKB 7.92). CYN 154806 TFA also blocks SRIF-induced increases [35S]-GTPγS binding in CHO-K1 cell membranes expressing human sst2 receptors as well as rat sst2(a) and rat sst2(b) receptors (pKB 7.81, 7.68 and 7.96, respectively).
CYN 154806 TFA (0.1 mg/kg; i.p.; 20 min before the administration of carbachol (CCh) (30 μg/kg) in M4 KO mice) dose-dependently and significantly reverses the decreases acid response to CCh in M4 but not M3 KO mice.
参考质量标准
外观:白色粉末纯度(HPLC) ≥98.0%
醋酸根含量≤12.0%
水分含量≤8.0%
肽含量≥80.0%
内毒素≤50EU/mg
氨基酸组成分析≤±10%