Angiopeptin TFA(Synonyms: 血管抑肽三氟乙酸盐)

Angiopeptin TFA;(Synonyms: 血管抑肽三氟乙酸盐) 纯度: 99.16%

Angiopeptin TFA 是生长抑素的环状八肽类似物,是一种 sst2/sst5 受体部分激动剂,IC50 值分别为 0.26 nM 和 6.92 nM。Angiopeptin TFA 可以抑制生长激素释放和胰岛素样生长因子-1 (IGF-1) 产生。Angiopeptin TFA 抑制腺苷酸环化酶或刺激细胞外酸化。Angiopeptin TFA 具有用于冠状动脉粥样硬化研究的潜力。

Angiopeptin TFAamp;;(Synonyms: 血管抑肽三氟乙酸盐)

Angiopeptin TFA Chemical Structure

CAS No. : 2478421-60-0

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Angiopeptin TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Neuronal Signaling Compound Library
  • Anti-Cardiovascular Disease Compound Library
  • Peptide Library

生物活性

Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research[1][2].

IC50 Target

IC50: 0.26 nM (sst2) and 6.92 nM (sst5)[1][2]

体外研究
(In Vitro)

Angiopeptin (0.1 nM- 10 μM; for 1 h) TFA acts as a partial agonist (pEC50=6.57) with a maximum response of 423% at 3 μM on the release of tritium on CHO hsst2 cells[2].

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

体内研究
(In Vivo)

Angiopeptin (20 and 50μg/kg; i.h.) TFA significantly inhibits neointimal formation[1].
Angiopeptin (20 μg/kg; per day) TFA significantly inhibits coronary artery myointimal proliferation in cardiac allografts by appmximalely 50%[1].

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

分子量

1326.39

Formula

C58H73F6N11O14S2

CAS 号

2478421-60-0

Sequence Shortening

{Nal}CYWKVCT-NH2

中文名称

血管抑肽三氟乙酸盐

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 : 10 mg/mL (7.54 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.7539 mL 3.7696 mL 7.5393 mL
5 mM 0.1508 mL 0.7539 mL 1.5079 mL
10 mM

*

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]. Lundergan CF, et al. Peptide inhibition of myointimal proliferation by angiopeptin, a somatostatin analogue. J Am Coll Cardiol. 1991;17(6 Suppl B):132B-136B.

    [2]. Alderton F, et al. Somatostatin receptor-mediated arachidonic acid mobilization: evidence for partial agonism of synthetic peptides. Br J Pharmacol. 2001;132(3):760-766.