CYN 154806 TFA

发表于由

CYN 154806 TFA; 纯度: 99.81%

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。

CYN 154806 TFAamp;;

CYN 154806 TFA Chemical Structure

规格 价格 是否有货 数量
1 mg ￥1800 In-stock
5 mg ￥5800 In-stock
10 mg ￥9800 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

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CYN 154806 TFA 相关产品

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生物活性

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].

IC50 Target

Somatostatin Receptor[1]
体外研究
(In Vitro)

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)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

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[3].

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

1311.36

Formula

C58H69F3N12O16S2
Sequence

Ac-Phe(4-NO2)-Cys-Tyr-Trp-Lys-Thr-Cys-Tyr-NH2 (Disulfide bridge: Cys2-Cys7)
Sequence Shortening

Ac-F(4-NO2)CYWKTCY-NH2 (Disulfide bridge: Cys2-Cys7)

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro:;

H2O : 25 mg/mL (19.06 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.7626 mL 3.8128 mL 7.6257 mL
5 mM 0.1525 mL 0.7626 mL 1.5251 mL
10 mM 0.0763 mL 0.3813 mL 0.7626 mL

*

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。
参考文献

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

    [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.

    [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.