Size | Price | Stock | Qty |
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500mg |
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1g |
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2g |
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5g |
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10g |
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25g |
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Other Sizes |
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Purity: ≥98%
Doxazosin mesylate (formerly UK-33274; UK 33274; trade names Cardura), the mesylate salt of Doxazosin which is a quinazoline-derivative, is a potent and selective antagonist of postsynaptic α1-adrenergic receptors (so called alpha-blockers) with anti-hypertensive effects. It can be used to treat benign prostatic hyperplasia-related high blood pressure and urinary retention. By blocking the binding of norepinephrine to the α-1 receptors on the membrane of vascular smooth muscle cells, doxazosin prevents the release of norepinephrine from sympathetic nerve terminals. The therapy of benign prostatic hyperplasia may be partially attributed to doxazosin's strong affinity for the alpha-1c adrenoceptor, which is the primary functional type in the prostate.
Targets |
α1-adrenergic receptor
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ln Vivo |
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Animal Protocol |
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References |
Molecular Formula |
C24H29N5O8S
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Molecular Weight |
547.58
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Exact Mass |
547.17
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Elemental Analysis |
C, 52.64; H, 5.34; N, 12.79; O, 23.37; S, 5.85
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CAS # |
77883-43-3
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Related CAS # |
Doxazosin; 74191-85-8; Doxazosin-d8 hydrochloride; 1219803-95-8
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Appearance |
Solid powder
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SMILES |
COC1=C(C=C2C(=C1)C(=NC(=N2)N3CCN(CC3)C(=O)C4COC5=CC=CC=C5O4)N)OC.CS(=O)(=O)O
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InChi Key |
VJECBOKJABCYMF-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C23H25N5O5.CH4O3S/c1-30-18-11-14-15(12-19(18)31-2)25-23(26-21(14)24)28-9-7-27(8-10-28)22(29)20-13-32-16-5-3-4-6-17(16)33-20;1-5(2,3)4/h3-6,11-12,20H,7-10,13H2,1-2H3,(H2,24,25,26);1H3,(H,2,3,4)
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Chemical Name |
[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(2,3-dihydro-1,4-benzodioxin-3-yl)methanone;methanesulfonic acid
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.57 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.8262 mL | 9.1311 mL | 18.2622 mL | |
5 mM | 0.3652 mL | 1.8262 mL | 3.6524 mL | |
10 mM | 0.1826 mL | 0.9131 mL | 1.8262 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT03339258 | Recruiting | Drug: Placebo Drug: Doxazosin Mesylate, Extended Release |
Stress Disorders, Post-Traumatic | San Francisco Veterans Affairs Medical Center |
April 15, 2018 | Phase 2 |
NCT05360953 | Recruiting | Drug: Clonidine Drug: Doxazosin Drug: Placebo |
Posttraumatic Stress Disorder | Charite University, Berlin, Germany |
April 6, 2022 | Phase 2 |
NCT04135846 | Recruiting | Drug: Doxazosin Drug: Placebo |
Alcohol Use Disorder (AUD) |
Brown University | December 19, 2019 | Phase 2 |
NCT01062945 | Completed | Drug: Placebo Drug: Doxazosin |
Cocaine Addiction Cocaine Abuse Cocaine Dependence Substance Abuse |
Scripps Health | January 2010 | Phase 1 |
NCT01145183 | Completed | Drug: Placebo Drug: Doxazosin |
Cocaine Dependence | Baylor College of Medicine | March 2010 | Phase 2 |
Effect of doxazosin on cell viability and apoptosis of malignant and benign prostate epithelial cells. Subconfluent cultures of PC-3 and BPH-1 cells were exposed to increasing concentrations of doxazosin (0–35 μmol/L) and cell death was determined using the MTT assay (A) or stained with Hoechst (B); apoptotic cells were visualized and counted as described in Materials and Methods. Cancer Res . 2006 Jan 1;66(1):464-72. td> |
Doxazosin causes an increase in Bax protein and induces caspase-8 activation in benign and malignant prostate epithelial cells. Cancer Res . 2006 Jan 1;66(1):464-72. td> |
Suppression of doxazosin-induced apoptosis by caspase-8 inhibitor. Cancer Res . 2006 Jan 1;66(1):464-72. td> |
Effect of doxazosin on the viability of HL-1 cardiomyocytes or NIH 3T3 cells. Circulation . 2003 Jan 7;107(1):127-31. td> |
Effect of doxazosin on primary cultures of cardiomyocytes. Circulation . 2003 Jan 7;107(1):127-31. td> |