1. Neuronal Signaling
  2. Cholinesterase (ChE) Amyloid-β
  3. Protriptyline

Protriptyline 是一种强效三环类抗抑郁剂 (TCA)。Protriptyline 可抑制乙酰胆碱酯酶 (AChE) 活性,IC50 值为 0.06 mM,并抑制 Aβ 自组装。Protriptyline 可用于抑郁症和阿尔茨海默病的研究。

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Protriptyline

Protriptyline Chemical Structure

CAS No. : 438-60-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Protriptyline is a potent tricyclic antidepressant (TCA). Protriptyline inhibits AChE activity with an IC50 value of 0.06 mM and inhibits Aβ self-assembly. Protriptyline can be used for the study of depression and Alzheimers disease[1][2][3].

IC50 & Target[1]

AChE

0.06 mM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
0.0017 μM
Compound: Protriptyline
Displacement of [3H]nisoxetine from human NET expressed in CHO cells after 120 mins by scintillation counting
Displacement of [3H]nisoxetine from human NET expressed in CHO cells after 120 mins by scintillation counting
[PMID: 22420844]
CHO IC50
2.8 nM
Compound: Protriptyline
Displacement of [3H]nisoxentine from human recombinant norepinephrine transporter expressed in CHO cells
Displacement of [3H]nisoxentine from human recombinant norepinephrine transporter expressed in CHO cells
[PMID: 26988801]
CHO IC50
2.8 x 10-9 M
Compound: Protriptyline
Displacement of [3H]nisoxetine from human recombinant norepinephrine transporter expressed in CHO cells measured after 120 mins by scintillation counting method
Displacement of [3H]nisoxetine from human recombinant norepinephrine transporter expressed in CHO cells measured after 120 mins by scintillation counting method
[PMID: 27876250]
HCC1954 EC50
> 10 μM
Compound: Protriptyline
Antiproliferative activity against human HCC1954 cells assessed as cell viability incubated for 72 hrs Alamar blue assay
Antiproliferative activity against human HCC1954 cells assessed as cell viability incubated for 72 hrs Alamar blue assay
[PMID: 31757681]
HCC1954 EC50
> 10 μM
Compound: Protriptyline
Induction of morphological changes in human HCC1954 cells assessed as number of nuclei incubated for 48 hrs by Hoechst 33342, SYTO14, Phalloidin-594, Wheat germ agglutinin-594, Concavalin-488, MitoTracker DeepRed staining based wide field fluorescent microscopic method
Induction of morphological changes in human HCC1954 cells assessed as number of nuclei incubated for 48 hrs by Hoechst 33342, SYTO14, Phalloidin-594, Wheat germ agglutinin-594, Concavalin-488, MitoTracker DeepRed staining based wide field fluorescent microscopic method
[PMID: 31757681]
T47D EC50
7.7 μM
Compound: Protriptyline
Induction of morphological changes in human T47D cells assessed as number of nuclei incubated for 48 hrs by Hoechst 33342, SYTO14, Phalloidin-594, Wheat germ agglutinin-594, Concavalin-488, MitoTracker DeepRed staining based wide field fluorescent microscopic method
Induction of morphological changes in human T47D cells assessed as number of nuclei incubated for 48 hrs by Hoechst 33342, SYTO14, Phalloidin-594, Wheat germ agglutinin-594, Concavalin-488, MitoTracker DeepRed staining based wide field fluorescent microscopic method
[PMID: 31757681]
T47D EC50
> 10 μM
Compound: Protriptyline
Antiproliferative activity against human T47D cells assessed as cell viability incubated for 72 hrs Alamar blue assay
Antiproliferative activity against human T47D cells assessed as cell viability incubated for 72 hrs Alamar blue assay
[PMID: 31757681]
体外研究
(In Vitro)

Protriptyline (0-70 μM;24 小时;PC3 细胞) 在 PC3 细胞中引起细胞毒性[2]

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

Cell Cytotoxicity Assay[2]

Cell Line: PC3 cells
Concentration: 50, 60 and 70 μM
Incubation Time: 24 hours
Result: Decreased cell viability in a concentration-dependent manner.
体内研究
(In Vivo)

Protriptyline (10 mg/kg;腹腔注射;21 天;AD 大鼠模型) 改善 STZ 处理大鼠的空间学习和保留记忆[3]

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

Animal Model: Rat model of AD[3]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; for 21 days.
Result: Reduced pTau, Aβ42 and BACE-1 levels, neurodegeneration, oxidative stress and glial activation. Improved p-ERK/ERK ratio and enhanced BDNF and CREB levels by reducing NFκB and GFAP expression.
Clinical Trial
分子量

263.38

Formula

C19H21N

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Protriptyline
目录号:
HY-B0949A
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