Colivelin TFA

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Colivelin TFA; 纯度: 99.22%

Colivelin TFA 是一种具有大脑通透性的神经保护肽 (neuroprotective peptide)，是 STAT3 的有效激活剂。Coliveli 通过激活 STAT3 在体外抑制神经元死亡。Colivelin TFA 对神经毒性、Aβ 沉积,神经元细胞凋亡，在神经退行性疾病显示出长期有利的影响。Colivelin TFA 可用于阿尔茨海默病和缺血性脑损伤的相关研究。

Colivelin TFAamp;;

Colivelin TFA Chemical Structure

规格 价格 是否有货 数量
500 μg ￥2280 In-stock
1 mg ￥3480 In-stock
5 mg ; 询价 ;
10 mg ; 询价 ;

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Colivelin TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro[1]. Colivelin TFA exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease[2]. Colivelin TFA has the potential for the treatment of alzheimer’s disease and ischemic brain injury[1].

IC50 Target[1]

STAT3

;

Amyloid-β

;

体外研究
(In Vitro)

Colivelin completely suppresses death induced by overexpressed FAD-causative genes and Aβ1-43 at a concentration of 100 fm, and keep its neuroprotective action at or above the levels of 1 nm[1].
Colivelin-induced neuroprotection occurs via two neuroprotective pathways: one mediated by Ca2+/calmodulin-dependent protein kinase IV, triggered by ADNF, and one mediated by signal transducer and activator of transcription 3, triggered by HN[1].
Colivelin reverses caspase3, Bax and Bcl-2 expressions in HT22 cells medaited by rmMFG-E8 in the co-cultured cells under OGD condition[4].
Colivelin (50 µg/mL, 4 hours) significantly increases the p-STAT3 protein levels in BV-2 cells[4].

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

Western Blot Analysis[4]

Cell Line: BV-2 cells.
Concentration: 50 µg/mL.
Incubation Time: 4 hours.
Result: Increased p-STAT3 levels.

Cell Viability Assay[5]

Cell Line: KYSE70 and TE8 cells.
Concentration: 0.5 μM.
Incubation Time: 1 hour (followed by CYT-Rx20 treatment)
Result: Significantly suppressed the viability in KYSE70 and TE8 cells.

体内研究
(In Vivo)

Colivelin(intracerebroventricular administration; 10 pmol/3 μl; 3 weeks) suppresses impairment in spatial working memory induced by repetitive intracerebroventricular injection of Aβ25-35 or Aβ1-42, in addition, it antagonizes neuronal loss in the CA1 region of hippocampus induced by hippocampal injection of Aβ1-42[1].
Colivelin (intraperitoneal administration; 1.4, 7, or 35 nM/0.21mL; on the Y-maze testday) suppresses memory impairment caused by 3-quinuclidinyl benzilateand restricts functional memory deficit[1].
Colivelin (intraperitoneal injection; 1 mg/kg; 14 days) results in improved motor and cognitive function with time by performance of mNSS, rotarod, and corner turning test.It also reduces lesion volume and improves neurological deficits after MCAO[1].

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

Animal Model: CD-1 mice[1]
Dosage: 10 pmol/3 μl
Administration: Intracerebroventricular administration
Result: Completely suppressed Aβ 25-35-mediated impairment in spatial working memory and increased the number of immunoreactive neurons.
Animal Model: C57 mice[1]
Dosage: 1.4, 7, or 35 nM/0.21mL
Administration: Intraperitoneal administration
Result: Protected against cholinotoxin-induced amnesia in mice.
Animal Model: Male C57BL/6 mice[3]
Dosage: 1 mg/kg
Administration: Intraperitoneal administration
Result: Protected against ischemic brain injury, and improves neurological outcomes.

分子量

2759.12

Formula

C119H206N32O35.C2HF3O2
Sequence Shortening

SALLRSIPAPAGASRLLLLTGEIDLP
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 : 50 mg/mL (18.12 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.3624 mL 1.8122 mL 3.6243 mL
5 mM 0.0725 mL 0.3624 mL 0.7249 mL
10 mM 0.0362 mL 0.1812 mL 0.3624 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：;Water with 5% sefsol and 20% isopropanol

    Solubility: 6.25 mg/mL (2.27 mM); Suspended solution; Need ultrasonic

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Chiba T, et al. Development of a femtomolar-acting humanin derivative named colivelin by attaching activity-dependent neurotrophic factor to its N terminus: characterization of colivelin-mediated neuroprotection against Alzheimer’s disease-relevant insults in vitro and in vivo. J Neurosci. 2005 Nov 2;25(44):10252-61.

    [2]. Zhao H, et al. Colivelin Rescues Ischemic Neuron and Axons Involving JAK/STAT3 Signaling Pathway.Neuroscience. 2019 Sep 15;416:198-206.

    [3]. Pan Z, et al. Upregulation of HSP72 attenuates tendon adhesion by regulating fibroblast proliferation and collagen production via blockade of the STAT3 signaling pathway.Cell Signal. 2020 Mar 18:109606.

    [4]. Fang YY, et al. MFG-E8 alleviates oxygen-glucose deprivation-induced neuronal cell apoptosis by STAT3 regulating the selective polarization of microglia. Int J Neurosci. 2020 Mar 12:1-10.

    [5]. Chiu WC, et al. The Synthetic β-Nitrostyrene Derivative CYT-Rx20 Inhibits Esophageal Tumor Growth and Metastasis via PI3K/AKT and STAT3 Pathways. PLoS One. 2016 Nov 22;11(11):e0166453.