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Purity: ≥98%
Terazosin HCl (A45975; A 45975; A-45975; Vasocard; Hyprin), the hydrochloride salt of Terazosin (racemate of terazosin), is a potent and selective α1-adrenoceptor antagonist which is used for treatment of symptoms of an enlarged prostate (BPH- benign prostatic hyperplasia). Terazosin produces cytotoxicity with an IC50 of greater than 100 μM in PC-3 and human benign prostatic cells. In cultured human umbilical vein endothelial cells, terazosin also effectively inhibited tube formation and vascular endothelial growth factor-induced proliferation (IC50 9.9 and 6.8 μM, respectively).
| Targets |
α1-adrenoceptor
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| Cell Assay |
In the current study, various identification techniques were employed to ascertain the mode of action of the cytotoxic effect. With terminal deoxynucleotidyl transferase deoxyuridine triphosphate nick end labeling, apoptotic cells can be identified in situ. After PC-3 cells were treated with 100 μM terazosin for 12 hours, the results indicate a positive response.
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| References |
| Molecular Formula |
C19H26CLN5O4
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| Molecular Weight |
423.9
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| Exact Mass |
423.17
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| Elemental Analysis |
C, 53.84; H, 6.18; Cl, 8.36; N, 16.52; O, 15.10
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| CAS # |
63074-08-8
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| Related CAS # |
Terazosin hydrochloride dihydrate; 70024-40-7; (R)-Terazosin; 109351-34-0; (S)-Terazosin; 109351-33-9; Terazosin; 63590-64-7
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| Appearance |
Solid powder
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| SMILES |
COC1=C(C=C2C(=C1)C(=NC(=N2)N3CCN(CC3)C(=O)C4CCCO4)N)OC.Cl
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| InChi Key |
IWSWDOUXSCRCKW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H25N5O4.ClH/c1-26-15-10-12-13(11-16(15)27-2)21-19(22-17(12)20)24-7-5-23(6-8-24)18(25)14-4-3-9-28-14;/h10-11,14H,3-9H2,1-2H3,(H2,20,21,22);1H
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| Chemical Name |
[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(oxolan-2-yl)methanone;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3590 mL | 11.7952 mL | 23.5905 mL | |
| 5 mM | 0.4718 mL | 2.3590 mL | 4.7181 mL | |
| 10 mM | 0.2359 mL | 1.1795 mL | 2.3590 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04551040 | Active Recruiting |
Drug: Terazosin | Healthy | University of Iowa | March 26, 2021 | Phase 1 |
| NCT04760860 | Not yet recruiting | Drug: Terazosin Hydrochloride Other: Placebo |
Dementia With Lewy Bodies | Qiang Zhang | October 2024 | Phase 1 Phase 2 |
| NCT04386317 | Recruiting | Drug: Terazosin | REM Sleep Behavior Disorder Pre-motor Parkinson's Disease |
Cedars-Sinai Medical Center | November 1, 2020 | Phase 2 |
| NCT05109364 | Recruiting | Drug: Terazosin therapy | REM Sleep Behavior Disorder Pre-motor Parkinson's Disease |
Cedars-Sinai Medical Center | September 23, 2022 | Phase 2 |
| NCT05855577 | Not yet recruiting | Drug: Terazosin | Parkinson Disease Gait Analysis Metabolic Disease |
I.R.C.C.S. Fondazione Santa Lucia |
December 2023 | Phase 4 |
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