Size | Price | Stock | Qty |
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250mg |
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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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Other Sizes |
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Purity: ≥98%
Doxazosin (UK 33274), a quinazoline-derivative, potently and selectively antagonizes postsynaptic α1-adrenergic receptors, used in the treatment of high blood pressure and urinary retention associated with benign prostatic hyperplasia. Doxazosin inhibits the binding of norepinephrine, which is released from sympathetic nerve terminals, to the α-1 receptors on the membrane of vascular smooth muscle cells. Doxazosin nt also shows high affinity to alpha-1c adrenoceptor, the predominant functional type in the prostate, which may partially attribute to its effect in treatment of benign prostatic hyperplasia.
ln Vitro |
Long-acting α1-adrenergic receptor inhibitors, such as doxazosin (UK 33274), are frequently used to treat symptoms of lower urinary tract and benign prostatic hyperplasia [1]. Doxazosin may directly suppress the synthesis of cholesterol without the need of LDL receptors. Doxazosin can suppress the synthesis of cholesterol, but cells may counteract this by upregulating LDL receptors. This would increase the import of lipoprotein cholesterol and decrease the amount of LDL cholesterol in the culture medium [2]. In 8 out of 12 patients (66.7%), doxazosin monotherapy was efficacious; in 11 out of 12 patients (91.7%), combination therapy with a beta-blocker was beneficial. Throughout the course of treatment, the average pulse rate did not change. Only three subjects experienced minor and temporary adverse effects. When taking doxazosin, urinary and plasma catecholamine levels usually drop or stay the same [3].
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References |
[1]. Sun, J.A., et al., Stereoselective binding of doxazosin enantiomers to plasma proteins from rats, dogs and humans in vitro. Acta Pharmacol Sin, 2013. 34(12): p. 1568-74.
[2]. D'Eletto, R.D. and N.B. Javitt, Effect of doxazosin on cholesterol synthesis in cell culture. J Cardiovasc Pharmacol, 1989. 13 Suppl 2: p. S1-4; discussion S4. [3]. Miura, Y. and K. Yoshinaga, Doxazosin: a newly developed, selective alpha 1-inhibitor in the management of patients with pheochromocytoma. Am Heart J, 1988. 116(6 Pt 2): p. 1785-9. |
Molecular Formula |
C23H25N5O5
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Molecular Weight |
451.48
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Exact Mass |
451.18557
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Elemental Analysis |
C, 61.19; H, 5.58; N, 15.51; O, 17.72
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CAS # |
74191-85-8
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Related CAS # |
Doxazosin mesylate;77883-43-3;Doxazosin-d8 hydrochloride;1219803-95-8;Doxazosin-d8;1126848-44-9
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
COC1=C(C=C2C(=C1)C(=NC(=N2)N3CCN(CC3)C(=O)C4COC5=CC=CC=C5O4)N)OC
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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
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Synonyms |
UK-33274 mesylateUK33274 mesylateUK 33274 mesylateCardura DoxazosinumDoxazosin Doxazosina Doxazosine Alfamedin Aliud Brand of Doxazosin Mesylate Alpharma Brand of Doxazosin Mesylate Almirall Brand of Doxazosin MesylateAlter Brand of Doxazosin Mesylate Apo Doxazosin Apo-Doxazosin
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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 |
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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2149 mL | 11.0747 mL | 22.1494 mL | |
5 mM | 0.4430 mL | 2.2149 mL | 4.4299 mL | |
10 mM | 0.2215 mL | 1.1075 mL | 2.2149 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.