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Purity: ≥98%
Terazosin HCl dihydrate (Hytrin; A-45975; A45975), the hydrochloride salt and dihydrated form of terazosin, is a potent and selective α1-adrenoceptor antagonist with antihypertensive effects. It has been applied to treat benign prostatic hyperplasia, or BPH (enlargening of the prostate) symptoms. In PC-3 and human benign prostatic cells, terazosin causes cytotoxicity with an IC50 greater than 100 μM. 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 |
α-adrenergic receptor
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| Cell Assay |
The present study employed multiple identification techniques to ascertain the mode of action of the cytotoxic effect. Use of terminal deoxynucleotidyl transferase deoxyuridine triphosphate nick end labeling allows for the in situ detection of apoptotic cells. Data indicate that PC-3 cells treated with 100 μM terazosin for 12 hours showed a positive response.
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| References |
| Molecular Formula |
C19H30CLN5O6
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| Molecular Weight |
459.92
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| Exact Mass |
387.19
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| Elemental Analysis |
C, 49.62; H, 6.57; Cl, 7.71; N, 15.23; O, 20.87
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| CAS # |
70024-40-7
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| Related CAS # |
(R)-Terazosin; 109351-34-0; (S)-Terazosin; 109351-33-9; Terazosin; 63590-64-7; Terazosin hydrochloride; 63074-08-8
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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.O.O.Cl
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| InChi Key |
NZMOFYDMGFQZLS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H25N5O4.ClH.2H2O/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;2*1H2
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| Chemical Name |
[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(oxolan-2-yl)methanone;dihydrate;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) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.44 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 4.55 mg/mL (9.89 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1743 mL | 10.8715 mL | 21.7429 mL | |
| 5 mM | 0.4349 mL | 2.1743 mL | 4.3486 mL | |
| 10 mM | 0.2174 mL | 1.0871 mL | 2.1743 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.
 Representative traces of urethral (a) and abdominal (b) pressure changes induced by duloxetine (1 mg/kg iv) in the presence of intrathecal (it) methiothepin maleate (A), terazosin (B), coapplication of methiothepin maleate and terazosin (C), and coapplication.Am J Physiol Renal Physiol. 2008 Jul; 295(1): F264–F271. |
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