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Chemical Structure| 63074-08-8 Chemical Structure| 63074-08-8

Structure of Terazosin HCl
CAS No.: 63074-08-8

Chemical Structure| 63074-08-8

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Terazosin HCl is a selective antagonist for alpha-adrenergic receptor, used for treatment for hypertension and prostate enlargement (BPH) through lowering the blood pressure with elimination half-life of ‎12 hours.

Synonyms: Terazosin (hydrochloride); Hytrin; A-45975

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Product Details of Terazosin HCl

CAS No. :63074-08-8
Formula : C19H26ClN5O4
M.W : 423.89
SMILES Code : O=C(N1CCN(C2=NC(N)=C3C=C(OC)C(OC)=CC3=N2)CC1)C4OCCC4.[H]Cl
Synonyms :
Terazosin (hydrochloride); Hytrin; A-45975
MDL No. :MFCD00467965
InChI Key :IWSWDOUXSCRCKW-UHFFFAOYSA-N
Pubchem ID :44383

Safety of Terazosin HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Terazosin HCl

GPCR

Isoform Comparison

Biological Activity

Target
  • α-adrenergic receptor

In Vitro:

Cell Line
Concentration Treated Time Description References
HeLa cells 1/2 MIC (2 mg/mL) 1 hour Evaluate the effect of Terazosin on S. Typhimurium invasion into HeLa cells. Terazosin significantly reduced bacterial invasion. Antibiotics (Basel). 2022 Mar 30;11(4):465
RAW264.7 macrophages 1/2 MIC (2 mg/mL) 16 hours Evaluate the effect of Terazosin on S. Typhimurium intracellular replication in macrophages. Terazosin significantly reduced bacterial intracellular replication. Antibiotics (Basel). 2022 Mar 30;11(4):465
RAW 264.7 cells 10 µM 18-24 hours TZ exhibited a protective effect against H2O2-induced apoptosis, as demonstrated by LDH release assay, active caspase-3 Western blot, and caspase activity assay. Nat Chem Biol. 2015 Jan;11(1):19-25
RAW 264.7 cells 10 µM 18-24 hours TZ suppressed apoptosis induced by LPS and IFN-γ, as verified by Annexin V staining and LDH release assay. Nat Chem Biol. 2015 Jan;11(1):19-25
Mouse embryonic stem cell-derived motor neurons (mESC-MNs) 0.625, 1.25, 2.5 µM 24 hours To evaluate the protective effect of Terazosin against oxidative stress-induced cell death, results showed Terazosin completely protected cells from death at the highest concentration EBioMedicine. 2022 Sep;83:104202
Human neuroblastoma cells 10 µM 24 hours Increased ATP content and reduced α-synuclein accumulation J Clin Invest. 2019 Oct 1;129(10):4539-4549
MIN6 cells 20 µM 24 hours Terazosin selectively activated GPR119, leading to increased cAMP and ATP synthesis, consequently enhancing insulin secretion. Cell Prolif. 2025 Mar;58(3):e13764
Caco-2 cells 10 and 100 nM 24 hours To evaluate the effect of Terazosin on cell viability under H2O2 and 2-DG-induced stresses, results showed that Terazosin significantly improved cell survival. Int J Mol Sci. 2021 Dec 30;23(1):416
Chromobacterium violaceum CV026 1/2 MIC (2 mg/mL) 24 hours Evaluate the effect of Terazosin on QS-controlled pigment production. Terazosin significantly reduced pigment release. Antibiotics (Basel). 2022 Mar 30;11(4):465
Hepatic microsomes 0.5, 1, 2, 5, 20, 50, 100 µM 30 minutes To determine the kinetic parameters (Vmax, Km, CLint) for the disappearance of terazosin in hepatic microsomes and evaluate the inhibitory effect of DA-8159 on its metabolism. Results showed that DA-8159 significantly reduced the metabolic rate of terazosin (Vmax decreased by 13.8%, CLint decreased by 62.0%). Br J Pharmacol. 2007 May;151(1):24-34

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice VTA 6-OHDA dopamine depletion model Oral administration via drinking water 0.03 mg/kg/day Daily administration for approximately 16 days To test the protective effect of Terazosin on PD-related cognitive dysfunction, results showed that Terazosin reduced interval timing variability in VTA dopamine-depleted mice NPJ Parkinsons Dis. 2023 Mar 2;9(1):32
Mice NAFPD model Intraperitoneal injection 1.5 mg/kg Daily for 6 weeks Terazosin treatment improved hyperglycemia, obesity, and pancreatic β-cell dysfunction in NAFPD mice. Cell Prolif. 2025 Mar;58(3):e13764
Female albino mice S. Typhimurium infection model Intraperitoneal injection 1/2 MIC (2 mg/mL) Single injection, observed for 5 days Evaluate the effect of Terazosin on S. Typhimurium pathogenesis. Terazosin significantly protected mice from S.Typhimurium pathogenesis. Antibiotics (Basel). 2022 Mar 30;11(4):465
Mice MPTP-induced PD model Intraperitoneal injection 10 μg/kg Once daily for 7 days Increased brain ATP levels, slowed or prevented neuron loss, partially restored dopamine levels and motor function J Clin Invest. 2019 Oct 1;129(10):4539-4549
Drosophila HS>rpr Drosophila model Oral 10 μM 24 hours TZ significantly improved the survival rate of HS>rpr flies, indicating its inhibitory effect on apoptosis. Nat Chem Biol. 2015 Jan;11(1):19-25
Zebrafish C9orf72 knockdown and TDP-43G348C overexpression models Added to water 2.5, 10, 50 µM From 6 hpf until analysis at 30 hpf To assess the ameliorative effect of Terazosin on motor neuron phenotypes, results showed Terazosin dose-dependently increased axon lengths EBioMedicine. 2022 Sep;83:104202
C57BL/6N mice DSS-induced ulcerative colitis and ethanol-induced gastric ulcer models Intraperitoneal injection (ulcerative colitis) and oral administration (gastric ulcer) 4 mg/kg/day (ulcerative colitis) and 1 mg/kg/day (gastric ulcer) Once daily for 7 days To evaluate the protective effects of Terazosin on ulcerative colitis and gastric ulcer, results showed that Terazosin significantly alleviated clinical symptoms and inflammatory responses. Int J Mol Sci. 2021 Dec 30;23(1):416
Sprague-Dawley rats Healthy male rats Intravenous and oral 5 mg/kg (i.v.); 5 mg/kg (p.o.) Single dose To evaluate the effect of DA-8159 on the pharmacokinetics and pharmacodynamics (blood pressure changes) of terazosin. Results showed that co-administration of DA-8159 and terazosin significantly increased the plasma concentration of terazosin (AUC increased by 57.4%-75.4%) and enhanced its blood pressure-lowering effect. Br J Pharmacol. 2007 May;151(1):24-34
SD rats and spontaneously hypertensive rats (SHRs) SD rats and SHRs Transdermal iontophoresis 7.5 mg/1.5 g TEH hydrogel 10 hours To evaluate the pharmacokinetic characteristics and antihypertensive effects of IDDS-TEH. Results showed that the blood concentration of IDDS-TEH was significantly higher than passive diffusion (p<0.05) and significantly reduced blood pressure in SHRs. Drug Deliv. 2021 Dec;28(1):454-462

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00000620 Atherosclerosis ... More >> Cardiovascular Diseases Hypercholesterolemia Hypertension Diabetes Mellitus, Type 2 Diabetes Mellitus Coronary Disease Less << Phase 3 Completed - United States, Minnesota ... More >> Minneapolis Medical Research Foundation Minneapolis, Minnesota, United States, 55404 United States, New York Columbia University New York, New York, United States, 10027 United States, North Carolina Wake Forest University Winston-Salem, North Carolina, United States, 27106 United States, Ohio Case Western Reserve University Cleveland, Ohio, United States, 44106 United States, Tennessee Veterans Affairs Memphis, Tennessee, United States, 38104 United States, Washington University of Washington Seattle, Washington, United States, 98195 Canada, Ontario McMaster University Hamilton, Ontario, Canada Less <<
NCT03339258 Stress Disorders, Post-Traumat... More >>ic Less << Phase 2 Recruiting June 2021 United States, California ... More >> San Francisco VA Medical Center Recruiting San Francisco, California, United States, 94121 Contact: Andrew Levihn-Coon, B.A.    415-221-4810 ext 23809    andrew.levihn-coon@va.gov Less <<
NCT01323998 - Completed - -
NCT00000620 - Completed - -
NCT00684489 Hypertension Not Applicable Completed - -
NCT01323998 - Completed - -
NCT01332487 - Completed - -
NCT01332487 - Completed - -
NCT03653845 Primary Aldosteronism ... More >> Hypertension Less << Phase 3 Recruiting January 1, 2020 China, Chongqing ... More >> The third hospital affiliated to the Third Military Medical University Recruiting Chongqing, Chongqing, China, 400042 Contact: Hongbo He, MD.    86-23-68757880    cqhehongbo@gmail.com    Principal Investigator: Zhiming Zhu, MD.          China The third hospital affiliated to the Third Military Medical University Recruiting Chongqing, China, 400042 Contact: Zhiming Zhu, MD, PhD    86-023-68705094    zhuzm@yahoo.com    Principal Investigator: Zhiming Zhu, MD, PhD Less <<
NCT01386983 - Completed - -
NCT01332435 - Completed - -
NCT01218243 Benign Prostatic Hyperplasia (... More >>BPH) Less << Phase 2 Completed - China ... More >> Guang'an Men Hospotal Affiliated to China Academy of Chinese Medical Sciences Beijing, China, 100053 Less <<
NCT01390870 - Completed - -
NCT01332435 - Completed - -
NCT02966717 Renal Insufficiency, Chronic ... More >> Nephrotic Syndrome Less << Phase 2 Active, not recruiting October 2021 China, Guangdong ... More >> Zhujiang Hospital, Southern Medical University Guangzhou, Guangdong, China, 510282 Less <<
NCT01390870 - Completed - -
NCT01218243 - Completed - -
NCT01386983 - Completed - -
NCT01435954 - Completed - -
NCT00438113 Atrial Fibrillation Phase 4 Completed - Canada, Nova Scotia ... More >> QE II Health Sciences Centre Halifax, Nova Scotia, Canada, B3H 3A7 Less <<
NCT02244333 - Completed - -
NCT00700583 Nocturia Not Applicable Completed - Korea, Republic of ... More >> Department of Urology, Seoul National University Hospital Seoul, Korea, Republic of, 110-744 Less <<
NCT02046395 Type 2 Diabetes ... More >> Hypertension Less << Phase 4 Recruiting December 2019 United States, Louisiana ... More >> Tulane University Health Sciences Center Recruiting New Orleans, Louisiana, United States, 70112 Contact: Bonnie L Katalenich, MPH    504-988-0200    bkatalen@tulane.edu    Principal Investigator: Tina Thethi, MD, MPH Less <<
NCT01508637 Cardiovascular Effects Not Applicable Unknown December 2015 United States, Washington ... More >> University of Washington Medical Center Recruiting Seattle, Washington, United States, 98195 Less <<
NCT00687388 Benign Prostatic Hyperplasia Phase 4 Withdrawn(in order to prepare ... More >>a new clinical trial to evaluate with pathological change) Less << - Korea, Republic of ... More >> Severance Hospital Seoul, Korea, Republic of, 120-752 Samsung Medical Center Seoul, Korea, Republic of, 135-710 Asan Medical Center Seoul, Korea, Republic of, 138-736 Less <<
NCT00693199 Lower Urinary Tract Symptoms ... More >> Hypertension Less << Not Applicable Completed - China, Anhui ... More >> Biomedicine Inistitute of Anhui Medical University Hefei, Anhui, China, 230032 Less <<
NCT01530243 Disorder of Urinary Stent Phase 2 Phase 3 Completed - Iran, Islamic Republic of ... More >> Imam Khomeini Hospital Urmia, Azerbaijan-gharbi, Iran, Islamic Republic of Less <<
NCT00563485 Prostatic Hyperplasia ... More >> Urinary Retention Less << Not Applicable Terminated - China ... More >> Prince of Wales Hospital Hong Kong, China Less <<
NCT01366664 Ejaculation Phase 1 Completed - United States, Alabama ... More >> Anniston, Alabama, United States United States, Arizona Tempe, Arizona, United States United States, California Costa Mesa, California, United States United States, Florida Miramar, Florida, United States United States, Tennessee Knoxville, Tennessee, United States United States, Texas Dallas, Texas, United States Less <<
NCT03195673 Carotid Artery Stenosis Phase 2 Recruiting December 15, 2019 China, Beijing ... More >> Beijing Anzhen Hospital Recruiting Beijing, Beijing, China, 100029 Contact: He Yin, MD          The Luhe Teaching Hospital of the Capital Medical University Recruiting Beijing, Beijing, China, 101100 Contact: Xiaokun Geng, MD Less <<
NCT02244255 Prostatic Hyperplasia Phase 4 Completed - -
NCT00237510 Antidepressant Induced Excessi... More >>ve Sweating Less << Not Applicable Completed - United States, Pennsylvania ... More >> Thomas Jefferson University Department of Psychiatry and Human Behavior Philadelphia, Pennsylvania, United States, 19107 Less <<
NCT00449683 Hyperhidrosis Phase 4 Completed - United States, Pennsylvania ... More >> Thomas Jefferson University, Department of Psychiatry Philadelphia, Pennsylvania, United States, 19107 Less <<
NCT01530243 - Completed - -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.80mL

2.36mL

1.18mL

23.59mL

4.72mL

2.36mL

References

 

Historical Records

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