Protriptyline
Based on 2 publication(s) in Google Scholar
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.
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- CAS No.: 438-60-8
- Formule: C19H21N
- Masse moléculaire:263.38
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Protriptyline
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Activité biologique
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AChE 0.06 mM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.0017 μM
Compound: Protriptyline
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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
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[PMID: 22420844] |
| CHO | IC50 |
2.8 nM
Compound: Protriptyline
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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
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[PMID: 26988801] |
| CHO | IC50 |
2.8 x 10-9 M
Compound: Protriptyline
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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
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[PMID: 27876250] |
| HCC1954 | EC50 |
>10 μM
Compound: Protriptyline
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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
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[PMID: 31757681] |
| HCC1954 | EC50 |
>10 μM
Compound: Protriptyline
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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 micr
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 micr
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[PMID: 31757681] |
| T47D | EC50 |
>10 μM
Compound: Protriptyline
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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
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[PMID: 31757681] |
| T47D | EC50 |
7.7 μM
Compound: Protriptyline
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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 microsc
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 microsc
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[PMID: 31757681] |
Protriptyline (0-70 μM; 24 hours; PC3 cells) causes cytotoxicity in PC3 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC3 cells
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Concentration:50, 60 and 70 μM
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Incubation Time:24 hours
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Result:Decreased cell viability in a concentration-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rat model of AD[3]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection; for 21 days.
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 438-60-8
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Masse moléculaire 263.38
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Formule C19H21N
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SMILES
CNCCCC1C2=CC=CC=C2C=CC3=CC=CC=C13
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Commun Signal
Tricyclic antidepressants induce liver inflammation by targeting NLRP3 inflammasome activation. [Abstract]2023 May 25;21(1):123. PMID: 37231437 -
Biochem Biophys Res Commun
Identification of the corticotropin-releasing factor receptor 1 antagonists as inhibitors of Chikungunya virus replication using a Gaussia luciferase-expressing subgenomic replicon. [Abstract]2022 Dec 31:637:181-188. PMID: 36403481
Pureté et documentation
Références
[2]. Chang HT, et, al. The mechanism of protriptyline-induced Ca2+ movement and non-Ca2+-triggered cell death in PC3 human prostate cancer cells. J Recept Signal Transduct Res. 2015;35(5):429-34. [Content Brief]
[3]. Tiwari V, et, al. Protriptyline improves spatial memory and reduces oxidative damage by regulating NFκB-BDNF/CREB signaling axis in streptozotocin-induced rat model of Alzheimer's disease. Brain Res. 2021 Mar 1;1754:147261. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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