| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Terazosin targets α1-adrenergic receptors, which are located on smooth muscle cells in the prostate, bladder neck, and vascular smooth muscle. By selectively blocking these receptors, terazosin relaxes smooth muscle tone, improving urine flow in patients with BPH and reducing peripheral vascular resistance in patients with hypertension. The compound shows selectivity for α1A receptors, which are predominant in the prostate.
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| ln Vitro |
Terazosin does not distinguish between the numerous clonal α1-adrenergic receptor subtypes that are temporarily expressed in COS cells [1].
In vitro, terazosin is a selective α1-adrenergic receptor antagonist. Its activity is assessed using radioligand binding assays to determine receptor affinity and functional assays to measure antagonism of α1 receptor-mediated responses. The compound's selectivity for α1A over other α1 subtypes and other receptor families is determined in receptor profiling studies. |
| ln Vivo |
In order to facilitate stone passage, terazosin may be administered to treat ureteral stones. Treatment for distal ureteral stones, particularly those larger than 5 mm, with terazosin has been reported to be both safe and efficacious [3].
In vivo, terazosin is used clinically for the treatment of benign prostatic hyperplasia and hypertension. It is administered orally once daily. In BPH, terazosin improves urine flow and reduces symptoms of urinary obstruction by relaxing smooth muscle in the prostate and bladder neck. In hypertension, it reduces blood pressure by decreasing peripheral vascular resistance. |
| Enzyme Assay |
In vitro receptor binding assays for terazosin measure its affinity for α1-adrenergic receptors using radioligand displacement techniques. Membranes prepared from cells expressing the receptors are incubated with a radiolabeled α1 receptor ligand and varying concentrations of the compound. The binding affinity (Ki) is calculated from competitive binding curves. Functional assays measure antagonism of α1 receptor-mediated calcium mobilization or other signaling readouts.
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| Cell Assay |
In vitro cell-based assays for terazosin use cells expressing α1-adrenergic receptors. Cells are treated with serial dilutions of the compound, and α1 receptor-mediated responses such as calcium mobilization or inositol phosphate accumulation are measured. The IC50 for inhibition of α1 responses is calculated from dose-response curves. Cell viability is assessed in parallel.
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| Animal Protocol |
In vivo animal models for terazosin include rat models of hypertension and models of BPH. The compound is administered orally, and its effects on blood pressure, heart rate, and prostate smooth muscle tone are evaluated. Pharmacodynamic studies measure α1 receptor occupancy and functional antagonism in target tissues.
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| ADME/Pharmacokinetics |
Tetrazosin hydrochloride has a molecular formula of C19H25N5O4 · HCl and a molecular weight of 423.90. The compound is administered orally once daily. It is soluble in water and other solvents. Pharmacokinetic parameters including half-life, bioavailability, and tissue distribution are documented in clinical studies. The compound is eliminated primarily via the liver.
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| Toxicity/Toxicokinetics |
The toxicity profile of terazosin includes dizziness, headache, and postural hypotension due to its vasodilatory effects. The compound is contraindicated in patients with known hypersensitivity to quinazolines. The compound is for research use only and not for human use. Appropriate safety precautions should be taken during handling.
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| References |
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| Additional Infomation |
Terazosin hydrochloride is the hydrochloride salt form of terazosin, a quinazoline derivative with adrenergic antagonistic effects. Terazosin hydrochloride selectively inhibits α1-adrenergic receptors, leading to vasodilation, thereby reducing peripheral vascular resistance, decreasing venous return to the heart, and reducing urethral resistance, which may improve urinary flow and symptoms associated with benign prostatic hyperplasia. Furthermore, terazosin can lower low-density lipoprotein (LDL) and triglyceride levels while increasing high-density lipoprotein (HDL) concentrations.
See also: Terazosin (with active fraction). Terazocin Hydrochloride (anhydrous) is the anhydrous hydrochloride salt form of terazosin, a selective α1-adrenergic receptor antagonist used for the treatment of benign prostatic hyperplasia and hypertension. The compound relaxes smooth muscle in the prostate and bladder neck, improving urine flow, and reduces peripheral vascular resistance, lowering blood pressure. Terazosin is used for research purposes. |
| Molecular Formula |
C19H26CLN5O4
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|---|---|
| Molecular Weight |
423.9
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| Exact Mass |
423.1673
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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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| PubChem CID |
44383
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
664.5±65.0 °C at 760 mmHg
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| Flash Point |
355.7±34.3 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.636
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| LogP |
-0.96
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
544
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(N1CCN(C2=NC(N)=C3C=C(OC)C(OC)=CC3=N2)CC1)C4OCCC4.[H]Cl
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| Synonyms |
Hyprin; Vasocard; Terazocin HCl
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~31.25 mg/mL (~73.72 mM)
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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.
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