183658-72-2
中文名稱
CYN 154806; CYN154806
英文名稱
CYN 154806
CAS
183658-72-2
分子式
C56H68N12O14S2
分子量
1197.34
MOL 文件
183658-72-2.mol
更新日期
2024/12/31 13:25:35
183658-72-2 結構式
基本信息
英文別名
CYN 154806CYANAMID 154806
CYN 154806
CYN154806
M.W. 1197.35 C56H68N12O14S2
CYN 154806 TRIFLUOROACETATE SALT
CYANAMID 154806 trifluoroacetate salt
AC-(4-NITRO)PHE-D-CYS-TYR-D-TRP-LYS-THR-CYS-D-TYR-NH2
D-Tyrosinamide, N-acetyl-4-nitro-L-phenylalanyl-D-cysteinyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-threonyl-L-cysteinyl-, cyclic (2→7)-disulfide
物理化學性質
沸點1656.2±65.0 °C(Predicted)
密度1.47±0.1 g/cm3(Predicted)
儲存條件−20°C
儲存條件−20°C
溶解度H2OPeptide Solubility and Storage Guidelines:1.??Calculate the length of the peptide.2.??Calculate the overall charge of the entire peptide according to the following table:3.??Recommended solution:
酸度系數(pKa)9.87±0.15(Predicted)
形態(tài)powder
顏色white to off-white
水溶解性Soluble to 1 mg/ml in water
常見問題列表
生物活性
CYN 154806 是一種環(huán)狀八肽，是一種強效的，選擇性生長抑素 sst2 受體的拮抗劑，其對人重組 sst2、sst1、sst3、sst4 和sst5 受體的 pIC50 值分別為 8.58、5.41、6.07、5.76 和 6.48。靶點
Somatostatin Receptor.
體外研究
CYN 154806 inhibits SRIF-induced increases in extracellular acidification (EAR) in CHO-K1 cells expressing human sst2 receptors (pKB 7.92). CYN 154806 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).
體內研究
CYN 154806 (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.