Terazosin
Based on 8 publication(s) in Google Scholar
Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin works by relaxing blood vessels and the opening of the bladder. Terazosin has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.28%
- No. CAS: 63590-64-7
- Fòrmula: C19H25N5O4
- Peso molecular:387.43
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Terazosin
More- Eur J Med Chem. 2024 Mar 5:267:116209. [Abstract]
- Cell Prolif. 2025 Mar;58(3):e13764. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Neurochem Int. 2021 Feb:143:104942. [Abstract]
- Kaohsiung J Med Sci. 2026 Jun 9:e70242.
- Res Sq. 2025 Mar 16.
- Research Square Preprint. 2022 Jul.
- Authorea. March 31, 2022.
Ver todos los productos específicos de isoformas Adrenergic Receptor
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Actividad biológica
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α adrenergic receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
1.73 nM
Compound: Terazosin
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Intrinsic activity at human alpha1B adrenergic receptor expressed in CHOK1 cells co-expressing aequorin assessed as inhibition of agonist induced calcium mobilization preincubated for 15 mins followed by agonist addition measured for 20 secs in presence o
Intrinsic activity at human alpha1B adrenergic receptor expressed in CHOK1 cells co-expressing aequorin assessed as inhibition of agonist induced calcium mobilization preincubated for 15 mins followed by agonist addition measured for 20 secs in presence o
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[PMID: 27658792] |
| HEK293 | IC50 |
23.7 μM
Compound: terazosin
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Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
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[PMID: 18788725] |
Terazosin does not discriminate cloned α1-adrenoceptor subtypes transiently expressed in COS cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 63590-64-7
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Appearance Solid
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Peso molecular 387.43
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Fòrmula C19H25N5O4
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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)C4OCCC4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (8)
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Journal Impact Factor
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Most Recent
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Eur J Med Chem
Novel inhibitors targeting the PGK1 metabolic enzyme in glycolysis exhibit effective antitumor activity against kidney renal clear cell carcinoma in vitro and in vivo. [Abstract]2024 Mar 5:267:116209. PMID: 38354523 -
Cell Prolif
Terazosin, a repurposed GPR119 agonist, ameliorates mitophagy and β-cell function in NAFPD by inhibiting MST1-Foxo3a signalling pathway. [Abstract]2025 Mar;58(3):e13764. PMID: 39413003 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Neurochem Int
Astroglial adrenoreceptors modulate synaptic transmission and contextual fear memory formation in dentate gyrus. [Abstract]2021 Feb:143:104942. PMID: 33340594 -
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Solvente y solubilidad
DMSO : 20 mg/mL (51.62 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)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (6.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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 (274 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Michel MC, et al. Drugs for treatment of benign prostatic hyperplasia: affinity comparison at cloned alpha 1-adrenoceptor subtypes and in human prostate. J Auton Pharmacol. 1996 Feb;16(1):21-8. [Content Brief]
[2]. Vincent J, et al. Pharmacological tolerance to alpha 1-adrenergic receptor antagonism mediated by terazosin in humans. J Clin Invest. 1992 Nov;90(5):1763-8. [Content Brief]
[3]. Ju M, et al. Efficacy of combination terazosin and nifedipine therapy in postoperative treatment of distal ureteral stones after transurethral ureteroscopic lithotripsy. J Int Med Res. 2020 Apr;48(4):300060520904851. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5811 mL | 12.9056 mL | 25.8111 mL | 64.5278 mL |
| 5 mM | 0.5162 mL | 2.5811 mL | 5.1622 mL | 12.9056 mL | |
| 10 mM | 0.2581 mL | 1.2906 mL | 2.5811 mL | 6.4528 mL | |
| 15 mM | 0.1721 mL | 0.8604 mL | 1.7207 mL | 4.3019 mL | |
| 20 mM | 0.1291 mL | 0.6453 mL | 1.2906 mL | 3.2264 mL | |
| 25 mM | 0.1032 mL | 0.5162 mL | 1.0324 mL | 2.5811 mL | |
| 30 mM | 0.0860 mL | 0.4302 mL | 0.8604 mL | 2.1509 mL | |
| 40 mM | 0.0645 mL | 0.3226 mL | 0.6453 mL | 1.6132 mL | |
| 50 mM | 0.0516 mL | 0.2581 mL | 0.5162 mL | 1.2906 mL |