CYN 154806 TFA 

CYN 154806 TFA, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC₅₀ values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively^[1][2].

CYN 154806 TFA 抑制表达人 sst2 受体 (pKB 7.92) 的 CHO-K1 细胞中 SRIF 诱导的细胞外酸化 (EAR) 增加。CYN 154806 TFA 还阻断 SRIF 诱导的 [35S]-GTPγS 在表达人 sst2 受体以及大鼠 sst2 (a) 和大鼠 sst2 (b) 受体 (pKB 分别为 7.81、7.68 和 7.96) 的 CHO-K1 细胞膜中的结合增加^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CYN 154806 TFA (0.1 mg/kg；腹腔注射；在 M4 KO 小鼠中给予卡巴胆碱 (CCh)? (30 μg/kg) 前 20 分钟) 呈剂量依赖性并显著逆转 M4 中对 CCh 的酸反应降低，但不逆转 M3 KO 中对 CCh 的酸反应降低小鼠^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1311.36

C₅₈H₆₉F₃N₁₂O₁₆S₂

2828432-46-6

固体

White to light yellow

Ac-{L-4-NO2-Phe}{D-CYS}-Tyr-{D-TRP}-Lys-Thr-Cys{D-TYR}-NH2?(Disulfide?bridge:?Cys2-Cys7)

Ac-{L-4-NO2-Phe}{D-CYS}Y{D-TRP}KTC{D-TYR}-NH2 (Disulfide bridge: Cys2-Cys7)

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

• [1]. Bass RT, et al. Identification and characterization of novel somatostatin antagonists. Mol Pharmacol. 1996 Oct;50(4):709-15.  [Content Brief]

  [2]. Feniuk W, et al. Selective somatostatin sst(2) receptor blockade with the novel cyclic octapeptide, CYN-154806. Neuropharmacology. 2000 Jun 8;39(8):1443-50.  [Content Brief]

  [3]. Takeuchi K, et al. Activation of Muscarinic Acetylcholine Receptor Subtype 4 Is Essential for Cholinergic Stimulation of Gastric Acid Secretion: Relation to D Cell/Somatostatin. Front Pharmacol. 2016 Aug 30;7:278.  [Content Brief]