中文名称:

CYN 154806; CYN154806

中文同义词:

英文名称:

CYN 154806

英文同义词:

CYN 154806;CYANAMID 154806;AC-(4-NITRO)PHE-D-CYS-TYR-D-TRP-LYS-THR-CYS-D-TYR-NH2;CYN 154806 TRIFLUOROACETATE SALT;CYANAMID 154806 trifluoroacetate salt;M.W. 1197.35 C56H68N12O14S2;CYN 154806; CYN154806;D-Tyrosinamide, N-acetyl-4-nitro-L-phenylalanyl-D-cysteinyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-threonyl-L-cysteinyl-, cyclic (2→7)-disulfide

CAS号:

183658-72-2

分子式:

C56H68N12O14S2

分子量:

1197.34

EINECS号:

相关类别:

环肽;Somatostatin receptor

Mol文件:

183658-72-2.mol

沸点 

1656.2±65.0 °C(Predicted)

密度 

1.47±0.1 g/cm3(Predicted)

储存条件 

−20°C

形态

powder

酸度系数(pKa)

9.87±0.15(Predicted)

颜色

white to off-white

生物活性

CYN 154806 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。

靶点

Somatostatin Receptor.

体外研究

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).

体内研究

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.

安全说明 

22-24/25

WGK Germany 

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