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Terazosin HCl Adrenergic Receptor antagonist

Name: Terazosin HCl
Brand: Selleck Chemicals
SKU: S4679
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S4679

Terazosin (Hytrin, Zayasel, Terazosine, Flumarc, Fosfomic, Blavin) is a selective alpha-1 antagonist used for treatment of symptoms of an enlarged prostate (BPH). It works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls.

Chemical Structure

Molecular Weight: 423.89

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Quality Control

Batch: Purity: 99.69%

99.69

Related Targets	CXCR Hedgehog/Smoothened PKA AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas GPR
Other Adrenergic Receptor Inhibitors	ICI 118551 Hydrochloride (Zenidolol) L755507 Yohimbine HCl Atipamezole Higenamine hydrochloride Detomidine HCl Naftopidil Demethyl-Coclaurine Buflomedil HCl Fenoterol hydrobromide

Solubility

In vitro
Batch:

DMSO : 84 mg/mL (198.16 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 1 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.2mg/ml (9.91mM)	Taking the 1 mL working solution as an example, add 50 μL of 84 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.6mg/ml (1.42mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	423.89	Formula	C₁₉H₂₅N₅O₄.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	63074-08-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Hytrin, Zayasel, Terazosine, Flumarc, Fosfomic, Blavin			Smiles	COC1=C(C=C2C(=C1)C(=NC(=N2)N3CCN(CC3)C(=O)C4CCCO4)N)OC.Cl

Mechanism of Action

Targets/IC₅₀/Ki	alpha1-AR
In vitro	Terazosin induces cytotoxicity in PC-3 and human benign prostatic cells with an IC50 of more than 100 μM. Terazosin also effectively inhibited vascular endothelial growth factor induced proliferation and tube formation in cultured human umbilical vein endothelial cells (IC50 9.9 and 6.8 μM, respectively).
In vivo	Terazosin produces a dose-dependent, complete inhibition of motor activity and catalepsy. Intraventricularly administered this antagonist protects striatal and cerebral cortical alpha 1 receptors but not striatal or cortical D1 receptors from in vivo alkylation by N-ethoxycarbonyl-2-ethoxy-1,2-dihydroxyquinoline. Intraventricular terazosin also produces hypothermia and a reduced respiratory rate suggestive of a reduced sympathetic outflow. Terazosin does not impair performance on a horizontal wire test or the ability to make co-ordinated movements in a swim test.Terazosin significantly inhibits vascular endothelial growth factor induced angiogenesis in nude mice with an IC50 of 7.9 μM, showing that it has a more potent anti-angiogenic than cytotoxic effect.
References	[1] http://onlinelibrary.wiley.com/doi/10.1046/j.1471-4159.2002.01170.x/abstract [2] https://pubmed.ncbi.nlm.nih.gov/10625064/ [3] https://pubmed.ncbi.nlm.nih.gov/12544352/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04760860	Not yet recruiting	Dementia With Lewy Bodies	Qiang Zhang\|University of Iowa	October 2024	Phase 1\|Phase 2
NCT04551040	Active not recruiting	Healthy	University of Iowa\|Michael J. Fox Foundation for Parkinson''s Research	March 26 2021	Phase 1
NCT04386317	Recruiting	REM Sleep Behavior Disorder\|Pre-motor Parkinson''s Disease\|Symptomatic Parkinson Disease	Cedars-Sinai Medical Center	November 1 2020	Phase 2
NCT00449683	Completed	Hyperhidrosis	Thomas Jefferson University\|National Alliance for Research on Schizophrenia and Depression	March 2007	Phase 4
NCT00237510	Completed	Antidepressant Induced Excessive Sweating	Thomas Jefferson University	May 2005	Not Applicable
NCT02244333	Completed	Prostatic Hyperplasia	Boehringer Ingelheim	February 2004	--

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