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TRAP-5 amide Sale

(Synonyms: SFLLR-NH2) 目录号 : GA23637

TRAP-5 amide,也称为SFLLR-amide,是一种蛋白酶激活受体1(PAR 1)激动剂肽。

TRAP-5 amide Chemical Structure

Cas No.:141923-41-3

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25mg
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100mg
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Sample solution is provided at 25 µL, 10mM.

Description

TRAP-5 amide, also known as SFLLR-amide, is a protease-activated receptor 1 (PAR 1) agonist peptide[1]. PAR 1 is the primary thrombin-responsive receptor in human cells and plays a significant role in tissue injury responses and related inflammation processes[2]. TRAP-5 amide mimics the action of thrombin and activates the thrombin receptor PAR 1 without the need for proteolysis, making it useful for studying PAR 1 activation mechanisms[3]. TRAP-5 amide is the smallest peptide that can release serotonin from human platelets and retain full activity, with the sequence Ser-Phe-Leu-Leu-Arg-NH2[4].

In vitro, treatment of A549 cells with TRAP-5 amide (10 μM) for 30 minutes under static conditions resulted in a positive dynamic mass redistribution (DMR) similar to that caused by a saturating dose of thrombin (10 units/ml), and this effect lasted for at least 2 hours. Additionally, TRAP-5 amide and thrombin showed mutual cross-desensitization[3].

References:
[1] Ceruso M A, McComsey D F, Leo G C, et al. Thrombin receptor-activating peptides (TRAPs): Investigation of bioactive conformations via structure–activity, spectroscopic, and computational studies[J]. Bioorganic & medicinal chemistry, 1999, 7(11): 2353-2371.
[2] Chen* C, Maryanoff* B E, Andrade-Gordon P. Thrombin receptor modulators: Medicinal chemistry, biological evaluation, and clinical application[J]. Thrombin: Physiology and Disease, 2009: 205-236.
[3] Goral V, Wu Q, Sun H, et al. Label-free optical biosensor with microfluidics for sensing ligand-directed functional selectivity on trafficking of thrombin receptor[J]. FEBS letters, 2011, 585(7): 1054-1060.
[4] Sabo T, Gurwitz D, Motola L, et al. Structure-activity studies of the thrombin receptor activating peptide[J]. Biochemical and biophysical research communications, 1992, 188(2): 604-610.

TRAP-5 amide,也称为SFLLR-amide,是一种蛋白酶激活受体1(PAR 1)激动剂肽[1]。PAR 1 是人体细胞中主要的凝血酶(thrombin)反应性受体,在组织损伤反应和相关炎症过程中发挥重要作用[2]。TRAP-5 amide模仿凝血酶的作用,无需蛋白水解即可激活凝血酶受体PAR 1,用于研究PAR 1激活机制[3]。TRAP-5 amide是能从人类血小板中释放血清素并保留全部活性的最小肽,序列为Ser-Phe-Leu-Leu-Arg-NH2[4]

在体外,TRAP-5 amide(10μM)处理A549细胞30 min,在静态条件下,饱和剂量的TRAP-5 amide(10μM)和凝血酶 (10unit/ml) 均导致类似的阳性 动态质量再分布(DMR),且至少持续 2小时。此外,TRAP-5 amide和凝血酶相互交叉脱敏[3]

实验参考方法

Cell experiment [1]:

Cell lines

A549 cells

Preparation method

The dynamic mass redistribution (DMR) of A549 cells responding to TRAP-5 amide (10μM) obtained under the static and flow conditions, continuous for 30 min.

Reaction Conditions

10μM; 30 min

Applications

Under the static stimulation condition both TRAP-5 amide (10μM) and thrombin (10unit/ml), each at a saturating dose, resulted in a similar positive-DMR that is sustained for at least 2 h.

References:
[1] Goral V, Wu Q, Sun H, et al. Label-free optical biosensor with microfluidics for sensing ligand-directed functional selectivity on trafficking of thrombin receptor[J]. FEBS letters, 2011, 585(7): 1054-1060.

化学性质

Cas No. 141923-41-3 SDF
别名 SFLLR-NH2
化学名 H-SER-PHE-LEU-LEU-ARG-NH2
分子式 C30H51N9O6 分子量 633.79
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mM 1.5778 mL 7.889 mL 15.7781 mL
5 mM 0.3156 mL 1.5778 mL 3.1556 mL
10 mM 0.1578 mL 0.7889 mL 1.5778 mL
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