Prazosin hydrochloride
Based on 17 publication(s) in Google Scholar
Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders. Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM.Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively.
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- Pureza: 99.89%
- No. CAS: 19237-84-4
- Fòrmula: C19H22ClN5O4
- Peso molecular:419.86
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) Prazosin hydrochloride
More- Nature. 2025 Dec;648(8092):146-156. [Abstract]
- Cancer Discov. 2026 Feb 9. [Abstract]
- Cell Discov. 2023 Feb 7;9(1):16. [Abstract]
- Cell Rep Med. 2024 Oct 1:101771. [Abstract]
- J Exp Med. 2023 Nov 6;220(11):e20230577. [Abstract]
- J Transl Med. 2022 Oct 2;20(1):444. [Abstract]
- Biomed Pharmacother. 2020 Apr;124:109731. [Abstract]
- Redox Rep. 2025 Dec;30(1):2494314. [Abstract]
- J Med Chem. 2021 Mar 11;64(5):2725-2738. [Abstract]
- Elife. 2024 May 29.
- Cells. 2023 May 24;12(11):1461. [Abstract]
- Drug Des Devel Ther. 2024 Apr 9:18:1103-1114. [Abstract]
- iScience. 2025 Jan 17;28(2):111831. [Abstract]
- Am J Pathol. 2023 Jul;193(7):913-926. [Abstract]
- Am J Physiol Renal Physiol. 2024 Nov 1;327(5):F885-F898. [Abstract]
- BMC Pulm Med. 2021 Jun 5;21(1):189. [Abstract]
- bioRxiv. 2024 November 03.
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Cell Proliferation/Viability Assay
Ver todos los productos específicos de isoformas Adrenergic Receptor
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Actividad biológica
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α adrenergic receptor |
Prazosin (0, 2.5, 5, 7.5, 10, 15, 20, 30, 40 and 50 μM) effectively inhibits the proliferation of U251 and U87 cells[4].
Prazosin inhibits the migration and invasion of U251 and U87 cells[4].
Prazosin treatment decreases the protein expression of components of the PI3K/AKT/mTOR signaling pathway. Prazosin (13.16 and 11.57 μM for U251 and U87 cells, 48 hours) decreases the expression levels of P70 and cyclin D1, which are downstream target genes of the PI3K/AKT/mTOR signaling pathway[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U251 and U87 cells
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Concentration:0, 2.5, 5, 7.5, 10, 15, 20, 30, 40 and 50 µM.
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Incubation Time:48 hours
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Result:The IC50s were 13.16±0.95 and 11.57±0.79 µM for U251 and U87 cells, respectively.
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Cell Line:U251 and U87 cells
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Concentration:13.16 and 11.57 µM for U251 and U87 cells, respectively
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Incubation Time:48 hours
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Result:Protein expression levels of Bax and active Caspase-3 were increased.
Bcl-2 levels were also decreased after prazosin treatment (P<0.05).
The expression of p-AKT and p-mTOR, P70 and cyclin D1 were decreased.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Fifty-five alcohol-naive male rats from the 60th generation of selective breeding for alcohol preference[1]
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Dosage:0.5, 1.0, 1.5, or 2.0 mg/kg
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Administration:Injected intraperitoneally (IP); 0.5 mg/mL; once a day at 15 min prior to onset of the daily two hour two-bottle choice, alcohol versus water, access period for two consecutive days and then three weeks later for five consecutive days.
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Result:Significantly reduced alcohol intake during the initial two daily administrations, and this reduction of alcohol intake was maintained for five consecutive days by daily prazosin treatment in the subsequent more prolonged trial.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 19237-84-4
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Appearance Solid
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Peso molecular 419.86
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Fòrmula C19H22ClN5O4
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Color White to off-white
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SMILES
O=C(N1CCN(C2=NC(N)=C3C=C(OC)C(OC)=CC3=N2)CC1)C4=CC=CO4.Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (17)
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Journal Impact Factor
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Most Recent
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Nature
2025 Dec;648(8092):146-156. PMID: 41094146 -
Cancer Discov
Myofibroblasts Induce Neuroplasticity to Promote Pancreatic Inflammation and Cancer Progression. [Abstract]2026 Feb 9. PMID: 41661076 -
Cell Discov
2023 Feb 7;9(1):16. PMID: 36746933 -
Cell Rep Med
The sympathetic nervous system drives hyperinflammatory responses to Clostridioides difficile infection. [Abstract]2024 Oct 1:101771. PMID: 39368481 -
J Exp Med
2023 Nov 6;220(11):e20230577. PMID: 37584653 -
J Transl Med
CDK1 serves as a therapeutic target of adrenocortical carcinoma via regulating epithelial-mesenchymal transition, G2/M phase transition, and PANoptosis. [Abstract]2022 Oct 2;20(1):444. PMID: 36184616 -
Biomed Pharmacother
Prazosin inhibits the proliferation and survival of acute myeloid leukaemia cells through down-regulating TNS1. [Abstract]2020 Apr;124:109731. PMID: 31954876
Prazosin hydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Apr;124:109731. [Abstract]
The expression of TNS1 in U937 and HL60 cells treated with different concentration of Prazosin is detected by Western blot analysis
Prazosin hydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Apr;124:109731. [Abstract]
Prazosin (5-15 μM) promoted apoptosis in HL60 and U937 cells in a dose-dependent manner under serum deprivation.
Prazosin hydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Apr;124:109731. [Abstract]
Cell proliferation was measured by the CCK-8 assay in U937 and HL60 cells treated with Prazosin (5-15 μM).
Prazosin hydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Apr;124:109731. [Abstract]
Prazosin (15 μM; 24 h) down-regulated the expression of all candidate genes except ABCD1 in U937 cells, with TNS1 being the most significantly down-regulated.
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Redox Rep
Norepinephrine promotes oxidative stress in vascular adventitial fibroblasts via PKC/NFκB-mediated NOX2 upregulation. [Abstract]2025 Dec;30(1):2494314. PMID: 40269356
Prazosin hydrochloride purchased from MedChemExpress. Usage Cited in: Redox Rep. 2025 Dec;30(1):2494314. [Abstract]
Prazosin (10 μM) abolished NE-induced increases in NOX2 expression in VAFs of Wistar-Kyoto rats (WKY) and spontaneously hypertensive rats (SHR).
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J Med Chem
Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration. [Abstract]2021 Mar 11;64(5):2725-2738. PMID: 33619967 -
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Cells
Impact of Short-Term (+)-JQ1 Exposure on Mouse Aorta: Unanticipated Inhibition of Smooth Muscle Contractility. [Abstract]2023 May 24;12(11):1461. PMID: 37296583 -
Drug Des Devel Ther
Dexmedetomidine Prolongs Lidocaine Intravenous Regional Anesthesia in Rats by Blocking the Hyperpolarization-Activated Cation Current. [Abstract]2024 Apr 9:18:1103-1114. PMID: 38618283 -
iScience
Stimulation of TRPV1+ peripheral somatosensory nerves suppress inflammation via the somato-autonomic reflex. [Abstract]2025 Jan 17;28(2):111831. PMID: 39967868 -
Am J Pathol
Hyperglycemia induces tear reduction and dry eye in diabetic mice through the norepinephrine-α1AR -mitochondrial impairment axis of lacrimal gland. [Abstract]2023 Jul;193(7):913-926. PMID: 37088455 -
Am J Physiol Renal Physiol
Anatomic and functional evidence for renal autonomic innervation in normotensive and hypertensive rats. [Abstract]2024 Nov 1;327(5):F885-F898. PMID: 39298550 -
BMC Pulm Med
Opposing responses of the rat pulmonary artery and vein to phenylephrine and other agents in vitro. [Abstract]2021 Jun 5;21(1):189. PMID: 34090386
Prazosin hydrochloride purchased from MedChemExpress. Usage Cited in: BMC Pulm Med. 2021 Jun 5;21(1):189. [Abstract]
Prazosin (2 mg/kg; i.p.; 60 min) abolished the inhibition of PAVA on TNF-α production in C57BL/6J male mice.
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Solvente y solubilidad
DMSO : 10 mg/mL (23.82 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 0.59 mg/mL (1.41 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.83 mg/mL (1.98 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.83 mg/mL (1.98 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (558 KB)
- English - EN (558 KB)
- Français - FR (558 KB)
- Deutsch - DE (558 KB)
- Norwegian - NO (558 KB)
- Español - ES (558 KB)
- Swedish - SV (558 KB)
- Italian - IT (558 KB)
- Portuguese - PT (558 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Dennis D Rasmussen, et al. The alpha1-adrenergic receptor antagonist, prazosin, reduces alcohol drinking in alcohol-preferring (P) rats. Alcohol Clin Exp Res. 2009 Feb;33(2):264-72. [Content Brief]
[2]. W S Colucci, et al. Nonlinear relationship between alpha 1-adrenergic receptor occupancy and norepinephrine-stimulated calcium flux in cultured vascular smooth muscle cells.Mol Pharmacol. 1985 May;27(5):517-24. [Content Brief]
[3]. Deborah L White, et al. OCT-1-mediated influx is a key determinant of the intracellular uptake of imatinib but not nilotinib (AMN107): reduced OCT-1 activity is the cause of low in vitro sensitivity to imatinib.Blood. 2006 Jul 15;108(2):697-704. [Content Brief]
[4]. Jing Zhang, et al. Prazosin inhibits the proliferation, migration and invasion, but promotes the apoptosis of U251 and U87 cells via the PI3K/AKT/mTOR signaling pathway. Exp Ther Med. 2020 Aug;20(2):1145-1152. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.3817 mL | 11.9087 mL | 23.8175 mL | 59.5437 mL |
| DMSO | 5 mM | 0.4763 mL | 2.3817 mL | 4.7635 mL | 11.9087 mL |
| 10 mM | 0.2382 mL | 1.1909 mL | 2.3817 mL | 5.9544 mL | |
| 15 mM | 0.1588 mL | 0.7939 mL | 1.5878 mL | 3.9696 mL | |
| 20 mM | 0.1191 mL | 0.5954 mL | 1.1909 mL | 2.9772 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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