Cat. No.: HY-B0098

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Doxazosin

(Synonyms: UK 33274)

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

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

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

Purity: 99.85%
CAS No.: 74191-85-8
Formula: C₂₃H₂₅N₅O₅
Molecular Weight:451.48

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)

Doxazosin Chemical Structure

CAS No.: 74191-85-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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

IC₅₀ & Target

α1-adrenergic receptors^[1]

All Adrenergic Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	7.73 μM Compound: DOXA	Antiproliferative activity against mouse 4T1 cells assessed as reduction in cell viability by MTT assay Antiproliferative activity against mouse 4T1 cells assessed as reduction in cell viability by MTT assay	[PMID: 38733884]
BT-549	IC₅₀	24.82 μM Compound: DOXA	Antiproliferative activity against human BT-549 cells assessed as reduction in cell viability by MTT assay Antiproliferative activity against human BT-549 cells assessed as reduction in cell viability by MTT assay	[PMID: 38733884]
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	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	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	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]
MDA-MB-231	IC₅₀	23.93 μM Compound: DOXA	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability by MTT assay	[PMID: 38733884]
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	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	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 SRB assay Cytotoxicity against human PC3 cells after 48 hrs by SRB assay	[PMID: 18817363]
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	>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	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	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]
PC-3	IC₅₀	45 μM Compound: Doxazosin	Inhibition of prostate cancer (PC-3) cell proliferation Inhibition of prostate cancer (PC-3) cell proliferation	[PMID: 15317457]

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 74191-85-8
Appearance Solid
Molecular Weight 451.48
Formula C₂₃H₂₅N₅O₅
Color White to off-white
SMILES

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

UK 33274
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)

Publications (3)

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Journal Impact Factor

Cancer Discov

Myofibroblasts Induce Neuroplasticity to Promote Pancreatic Inflammation and Cancer Progression. [Abstract]

2026 Feb 9. PMID: 41661076
Drug Deliv Transl Res

Sex-specific formulations of doxazosin mesylate via direct powder extrusion 3D printing. [Abstract]

2025 Apr 22. PMID: 40263229
PLoS Negl Trop Dis

Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]

2019 Aug 20;13(8):e0007681. PMID: 31430351

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (923 KB)
- English - EN (923 KB)
- Français - FR (923 KB)
- Deutsch - DE (923 KB)
- Norwegian - NO (923 KB)
- Español - ES (923 KB)
- Swedish - SV (923 KB)
- Italian - IT (923 KB)
- Korean - KR (923 KB)
- Portuguese - PT (923 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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

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Doxazosin

GPCR/G Protein Compound Library

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Publications Citing Use of MedChemExpress (MCE) Doxazosin

All Adrenergic Receptor Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Doxazosin Related Classifications

HY-B0098 Related Classifications