Home Neuronal Signaling Adrenergic Receptor antagonist Terazosin HCl Dihydrate

research use only

Terazosin HCl Dihydrate Adrenergic Receptor antagonist

Cat.No.S2059

Terazosin HCl is a selective α1-adrenoceptor antagonist, used for treatment of symptoms of an enlarged prostate (BPH).
Terazosin HCl Dihydrate Adrenergic Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 459.92

Jump to

Quality Control

Batch: S205901 DMSO]26 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.97%
99.97

Solubility

In vitro
Batch:

DMSO : 26 mg/mL (56.53 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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

mg/kg
g
μL

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 459.92 Formula

C19H25N5O4.HCl.2H2O

 Storage (From the date of receipt)
CAS No. 70024-40-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles COC1=C(C=C2C(=C1)C(=NC(=N2)N3CCN(CC3)C(=O)C4CCCO4)N)OC.O.O.Cl

Mechanism of Action

Targets/IC50/Ki
α-adrenergic receptor
In vitro
Terazosin results in a significant loss of cell viability, via induction of apoptosis in a dose-dependent manner in prostate cancer cells. Terazosin suppresses prostate growth potentially via α 1-adrenoceptor-independent actions gains further support from another study documenting that Doxazosin inhibits proliferation of human vascular smooth muscle cells independently of an antagonistic effect on α1-adrenoceptor. Terazosin blocks HERG currents in Xenopus oocytes with IC50 of 113.2 mM, while Terazosin blocks HERG channel inhibition in human HEK 293 cells with IC50 of 17.7 mM. Terazosin or genistein treatment inhibits the growth of DU-145 cells in a dose-dependent manner, whereas has no effect on normal prostate epithelial cells. Terazosin results in the genistein-induced arrest of DU-145 cells in G2/M phase being overridden and an increase in apoptotic cells, as evidenced by procaspase-3 activation and PARP cleavage. Terazosin induces cytotoxicity in PC-3 and human benign prostatic cells with an IC50 of more than 100 mM.
In vivo
Terazosin significantly inhibits vascular endothelial growth factor induced angiogenesis in nude mice with an IC50 of 7.9 mM, showing that it has a more potent anti-angiogenic than cytotoxic effect. Terazosin also effectively inhibits vascular endothelial growth factor induced proliferation and tube formation in cultured human umbilical vein endothelial cells (IC50 9.9 and 6.8 mM, respectively).
References
  • [4] 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 --

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Signaling Pathway Map