Doxazosin (Synonyms: UK 33274)

Name: Doxazosin
Brand: MedChemExpress
SKU: HY-B0098
Rating: 4.5 (1 reviews)

Cat. No.: HY-B0098 Purity: 99.85%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

Doxazosin (UK 33274) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors.

For research use only. We do not sell to patients.

Doxazosin Chemical Structure

CAS No. : 74191-85-8

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Doxazosin:

1 Publications Citing Use of MCE Doxazosin

•PLoS Negl Trop Dis. 2019 Aug 20;13(8):e0007681. [Abstract]

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α adrenergic receptor β adrenergic receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

Doxazosin (UK 33274) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors.

IC₅₀ & Target

α1-adrenergic receptors^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
DU-145	EC₅₀	> 100 μM Compound: doxazosin	Cytotoxicity against human DU145 cells after 72 hrs by CellTitter-Glo luminescent cell viability assay Cytotoxicity against human DU145 cells after 72 hrs by CellTitter-Glo luminescent cell viability assay	[PMID: 19719240]
DU-145	EC₅₀	100 μM Compound: doxazosin	Induction of apoptosis in human DU145 cells assessed as caspase 3/7 activation after 24 hrs Caspase-Glo 3/7 assay Induction of apoptosis in human DU145 cells assessed as caspase 3/7 activation after 24 hrs Caspase-Glo 3/7 assay	[PMID: 19719240]
DU-145	IC₅₀	30.56 μM Compound: Doxazosin	Antiproliferative activity against human DU145 cells after 120 hrs by MTT assay Antiproliferative activity against human DU145 cells after 120 hrs by MTT assay	[PMID: 28499171]
DU-145	IC₅₀	37.44 μM Compound: doxazosin	Cytotoxicity against human DU145 cells after 72 hrs by CellTitter-Glo luminescent cell viability assay Cytotoxicity against human DU145 cells after 72 hrs by CellTitter-Glo luminescent cell viability assay	[PMID: 19719240]
DU-145	IC₅₀	37.67 μM Compound: Doxazosin	Cytotoxicity against human DU145 cells after 48 hrs by WST-8 assay Cytotoxicity against human DU145 cells after 48 hrs by WST-8 assay	[PMID: 25874333]
HEK293-A	IC₅₀	19 μM Compound: doxazosin	Cytotoxicity against HEK293A cells transfected with alpha-1A adrenergic receptor assessed as cell viability by sulforhodamine B assay Cytotoxicity against HEK293A cells transfected with alpha-1A adrenergic receptor assessed as cell viability by sulforhodamine B assay	[PMID: 26005522]
HEK293-A	IC₅₀	22 μM Compound: doxazosin	Cytotoxicity against HEK293A cells transfected with alpha-1D adrenergic receptor assessed as cell viability by sulforhodamine B assay Cytotoxicity against HEK293A cells transfected with alpha-1D adrenergic receptor assessed as cell viability by sulforhodamine B assay	[PMID: 26005522]
LNCaP	IC₅₀	10.48 μM Compound: Doxazosin	Antiproliferative activity against human LNCAP cells after 120 hrs by MTT assay Antiproliferative activity against human LNCAP cells after 120 hrs by MTT assay	[PMID: 28499171]
LNCaP	EC₅₀	100 μM Compound: doxazosin	Induction of apoptosis in human LNCAP cells assessed as caspase 3/7 activation after 24 hrs Caspase-Glo 3/7 assay Induction of apoptosis in human LNCAP cells assessed as caspase 3/7 activation after 24 hrs Caspase-Glo 3/7 assay	[PMID: 19719240]
LNCaP	IC₅₀	27.89 μM Compound: Doxazosin	Cytotoxicity against human LNCAP cells after 48 hrs by WST-8 assay Cytotoxicity against human LNCAP cells after 48 hrs by WST-8 assay	[PMID: 25874333]
LNCaP	IC₅₀	28.11 μM Compound: doxazosin	Cytotoxicity against human LNCAP cells after 72 hrs by CellTitter-Glo luminescent cell viability assay Cytotoxicity against human LNCAP cells after 72 hrs by CellTitter-Glo luminescent cell viability assay	[PMID: 19719240]
NHDF	EC₅₀	100 μM Compound: doxazosin	Induction of apoptosis in human NHDF cells assessed as caspase 3/7 activation after 24 hrs Caspase-Glo 3/7 assay Induction of apoptosis in human NHDF cells assessed as caspase 3/7 activation after 24 hrs Caspase-Glo 3/7 assay	[PMID: 19719240]
NHDF	EC₅₀	40.4 μM Compound: doxazosin	Cytotoxicity against human NHDF cells after 72 hrs by CellTitter-Glo luminescent cell viability assay Cytotoxicity against human NHDF cells after 72 hrs by CellTitter-Glo luminescent cell viability assay	[PMID: 19719240]
NHDF	IC₅₀	43 μM Compound: doxazosin	Cytotoxicity against human NHDF cells after 72 hrs by CellTitter-Glo luminescent cell viability assay Cytotoxicity against human NHDF cells after 72 hrs by CellTitter-Glo luminescent cell viability assay	[PMID: 19719240]
PC-3	EC₅₀	> 100 μM Compound: doxazosin	Cytotoxicity against human PC3 cells after 72 hrs by CellTitter-Glo luminescent cell viability assay Cytotoxicity against human PC3 cells after 72 hrs by CellTitter-Glo luminescent cell viability assay	[PMID: 19719240]
PC-3	IC₅₀	> 50 μM Compound: Doxazosin	Cytotoxicity against human PC3 cells after 48 hrs by WST-8 assay Cytotoxicity against human PC3 cells after 48 hrs by WST-8 assay	[PMID: 25874333]
PC-3	EC₅₀	100 μM Compound: doxazosin	Induction of apoptosis in human PC3 cells assessed as caspase 3/7 activation after 24 hrs by Caspase-Glo 3/7 assay Induction of apoptosis in human PC3 cells assessed as caspase 3/7 activation after 24 hrs by Caspase-Glo 3/7 assay	[PMID: 19719240]
PC-3	IC₅₀	12.1 μM Compound: Doxazosin	Antiproliferative activity against human PC3 cells after 120 hrs by MTT assay Antiproliferative activity against human PC3 cells after 120 hrs by MTT assay	[PMID: 28499171]
PC-3	GI₅₀	26.9 μM Compound: Doxazosin	Cytotoxicity against human PC3 cells after 48 hrs by SRB assay Cytotoxicity against human PC3 cells after 48 hrs by SRB assay	[PMID: 18817363]
PC-3	GI₅₀	26.9 μM Compound: Doxazosin	Cytotoxic activity on human PC3 prostate cancer cells by SRB assay Cytotoxic activity on human PC3 prostate cancer cells by SRB assay	[PMID: 16302814]
PC-3	GI₅₀	26.9 μM Compound: Doxazosin	Cytotoxicity against human PC3 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human PC3 cells after 48 hrs by sulforhodamine B assay	[PMID: 23252794]
PC-3	IC₅₀	38.6 μM Compound: doxazosin	Cytotoxicity against human PC3 cells after 72 hrs by CellTitter-Glo luminescent cell viability assay Cytotoxicity against human PC3 cells after 72 hrs by CellTitter-Glo luminescent cell viability assay	[PMID: 19719240]

In Vitro

Doxazosin(UK 33274) is a long-lasting inhibitor of α1-adrenoceptors that is widely used to treat benign prostatic hyperplasia and lower urinary tract symptoms^[1]. doxazosin may have a direct inhibitory effect on cholesterol synthesis independent of the LDL receptor. The inhibition of cholesterol synthesis by doxazosin may cause cells to compensate by upregulating the LDL receptor, thereby increasing the importation of lipoprotein cholesterol and reducing LDL cholesterol in the medium^[2]. Doxazosin monotherapy was effective in eight of 12 patients (66.7%), and combined therapy with a beta-blocker was effective in 11 of 12 patients (91.7%). The mean pulse rate remained constant throughout therapy. Adverse reactions were minor and transient and occurred in only three patients. Urinary and plasma catecholamine levels tended to decrease or remained unchanged during doxazosin therapy^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

451.48

Formula

C₂₃H₂₅N₅O₅

CAS No.

74191-85-8

Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCN(C2=NC(N)=C3C=C(OC)C(OC)=CC3=N2)CC1)C4OC5=CC=CC=C5OC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (221.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.54 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.85%

Select Batch:

Data Sheet (275 KB) SDS (863 KB)

COA (250 KB) HNMR (271 KB) RP-HPLC (260 KB) LCMS (115 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2149 mL	11.0747 mL	22.1494 mL	55.3734 mL
	5 mM	0.4430 mL	2.2149 mL	4.4299 mL	11.0747 mL
	10 mM	0.2215 mL	1.1075 mL	2.2149 mL	5.5373 mL
	15 mM	0.1477 mL	0.7383 mL	1.4766 mL	3.6916 mL
	20 mM	0.1107 mL	0.5537 mL	1.1075 mL	2.7687 mL
	25 mM	0.0886 mL	0.4430 mL	0.8860 mL	2.2149 mL
	30 mM	0.0738 mL	0.3692 mL	0.7383 mL	1.8458 mL
	40 mM	0.0554 mL	0.2769 mL	0.5537 mL	1.3843 mL
	50 mM	0.0443 mL	0.2215 mL	0.4430 mL	1.1075 mL
	60 mM	0.0369 mL	0.1846 mL	0.3692 mL	0.9229 mL
	80 mM	0.0277 mL	0.1384 mL	0.2769 mL	0.6922 mL
	100 mM	0.0221 mL	0.1107 mL	0.2215 mL	0.5537 mL

Doxazosin Related Classifications

Endocrinology Cardiovascular Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Doxazosin74191-85-8UK 33274UK33274UK-33274Adrenergic ReceptorBeta ReceptorInhibitorinhibitorinhibit

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Doxazosin (Synonyms: UK 33274)

Customer Review

Other Forms of Doxazosin:

Doxazosin Related Antibodies

1 Publications Citing Use of MCE Doxazosin

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Adrenergic Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Doxazosin Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Doxazosin Related Classifications

Keywords:

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