Pep2m, myristoylated TFA(Synonyms: Myr-Pep2m TFA)

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Pep2m, myristoylated TFA;(Synonyms: Myr-Pep2m TFA) 纯度: 99.77%

Pep2m, myristoylated TFA (Myr-Pep2m TFA) 是一种细胞通透性肽。Pep2m, myristoylated TFA 能破坏蛋白激酶 ζ (PKMζ) 下游靶点 NSF/GluR2 相互作用。PKMζ 具有自主活性的 PKC 同工酶。

Pep2m, myristoylated TFAamp;;(Synonyms: Myr-Pep2m TFA)

Pep2m, myristoylated TFA Chemical Structure

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5 mg ￥3500 In-stock
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生物活性

Pep2m, myristoylated TFA (Myr-Pep2m TFA) is a cell-permeable peptide. Pep2m, myristoylated TFA can disrupt the protein kinase ζ (PKMζ) downstream targets, N-ethylmaleimide-sensitive factor/glutamate receptor subunit 2 (NSF/GluR2) interactions. PKMζ is an autonomously active isozyme of protein kinase C (PKC)[1][2].

IC50 Target

NSF/GluR2 interactions[1]
体外研究
(In Vitro)

Pep2m, myristoylated TFA (10 μM) blocks PKMζ-mediated AMPA receptor (AMPAR) potentiation[1].
Pep2m, myristoylated TFA does not block the increase of PKMζ in the hippocampal slices during long-term potentiation (LTP) maintenance, indicating that blocking NSF/GluR2 interactions do not prevent the induction of PKMζ synthesis[1].
Pep2m, myristoylated TFA blocks NSF/GluR2-mediated AMPAR trafficking, and reverses persistent potentiation at both the strongly stimulates synapses and the weakly stimulats synapses that underwent synaptic tagging and capture[1].

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

Pep2m, myristoylated TFA (10 µg/20 µL) results in an increase in paw withdrawal thresholds (PWTs) on nociceptive responses in the formalin test[2].

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

Animal Model: Female and male Long-Evans hooded rats (8 weeks)[2]
Dosage: 10 µg (in 20 µL)
Administration: Intrathecal injection
Result: Resulted in an increase in PWTs, in both male and female rats at various time points tested.

分子量

1497.83

Formula

C65H119F3N18O16S
Sequence Shortening

{Myr}-KRMKVAKNAQ
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:;

DMSO : 33.33 mg/mL (22.25 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.6676 mL 3.3382 mL 6.6763 mL
5 mM 0.1335 mL 0.6676 mL 1.3353 mL
10 mM 0.0668 mL 0.3338 mL 0.6676 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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (1.67 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.67 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.5 mg/mL (1.67 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.67 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Yudong Yao, et al. PKMζ Maintains Late Long-Term Potentiation by N-Ethylmaleimide-Sensitive Factor/GluR2-Dependent Trafficking of Postsynaptic AMPA Receptors. J Neurosci. 2008 Jul 30; 28(31): 7820-7827.

    [2]. Nicole C George, et al. Sex differences in the contributions of spinal atypical PKCs and downstream targets to the maintenance of nociceptive sensitization. Mol Pain. 2019; 15: 1744806919840582.