| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Bunazosin targets the α1-adrenoceptor (α1-adrenoceptor), a G protein-coupled receptor that mediates vasoconstriction in vascular smooth muscle. By blocking α1-adrenoceptors, bunazosin relaxes vascular smooth muscle, leading to vasodilation and reduced blood pressure. The compound is a potent and specific antagonist, and its mechanism of action involves competitive antagonism of norepinephrine and epinephrine at α1-adrenoceptors.
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| ln Vitro |
Bunazosin is a potent and specific α1-adrenoceptor antagonist. By blocking α1-adrenoceptors in vascular smooth muscle, it helps relax blood vessels, reducing blood pressure. The compound has been used in clinical trials for the treatment of hypertension. Its activity against benign prostatic hyperplasia is related to relaxation of smooth muscle in the prostate and bladder neck. Specific IC50 values and detailed activity data are not extensively documented.
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| ln Vivo |
In vivo, bunazosin is used primarily to treat hypertension and benign prostatic hyperplasia (BPH). It lowers blood pressure by blocking α1-adrenoceptors in vascular smooth muscle, leading to vasodilation. The compound has been used in clinical trials for the treatment of hypertension. It may also be used in intraocular pressure-lowering studies. Bunazosin is administered orally and has demonstrated efficacy in clinical settings.
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| Enzyme Assay |
The in vitro receptor binding assay for Bunazosin typically involves measuring its affinity for the α1-adrenoceptor using radioligand binding. Membrane preparations from cells expressing α1-adrenoceptors are incubated with varying concentrations of bunazosin (typically 0.001-100 µM) and a radiolabeled ligand such as [3H]prazosin. The binding affinity is determined by competition binding analysis. The compound is dissolved in DMSO and diluted in assay buffer.
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| Cell Assay |
In vitro cellular assays for Bunazosin typically involve treating cells expressing α1-adrenoceptors with the compound at concentrations ranging from 0.001 to 10 µM. Receptor antagonism is assessed by measuring the inhibition of α1-adrenoceptor-mediated signaling, such as calcium mobilization or inositol phosphate production. The compound's ability to block agonist-induced responses is evaluated. Cell viability is assessed using MTT or other standard assays. The compound is dissolved in DMSO and diluted in cell culture medium.
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| Animal Protocol |
In vivo animal studies for Bunazosin typically involve administration to rats or rabbits via oral gavage or intravenous injection at doses determined from preliminary studies. Blood pressure is measured using invasive or non-invasive methods. Intraocular pressure is measured using tonometry. The compound's effects on blood pressure, heart rate, and intraocular pressure are evaluated. Blood and tissue samples are collected for pharmacokinetic and pharmacodynamic analysis.
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| ADME/Pharmacokinetics |
Bunazosin has a molecular weight of 373.45 g/mol and formula C19H27N5O3. It is soluble in DMSO (~100 mg/mL, ~267.77 mM). Recommended storage is powder at -20°C for up to 3 years and at 4°C for up to 2 years. The compound appears as an off-white to yellow solid powder with purity ≥98%. Detailed PK parameters such as half-life, Cmax, AUC, and bioavailability would require experimental determination.
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| Toxicity/Toxicokinetics |
Bunazosin is intended for research use only and is not approved for human therapeutic applications in this context. As an α1-adrenoceptor antagonist, it may cause hypotension, dizziness, and other cardiovascular effects. Standard preclinical toxicity assessments would include acute toxicity studies in rodents, repeated-dose toxicity studies, and assessment of off-target effects. The compound's antihypertensive effects suggest it may have cardiovascular effects.
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| Additional Infomation |
Bunazosin belongs to the quinazoline class of drugs. Bunazosin has been used in clinical trials for the treatment of hypertension.
Bunazosin (CAS 80755-51-7) is a potent and specific α1-adrenoceptor antagonist with a molecular weight of 373.45 g/mol and formula C19H27N5O3. It is used primarily to treat hypertension and benign prostatic hyperplasia (BPH) and has been used in clinical trials. Bunazosin belongs to the quinazoline class of drugs and is also known as 布纳唑嗪. It is not approved for clinical use in this context. |
| Molecular Formula |
C19H27N5O3
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|---|---|
| Molecular Weight |
373.4494
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| Exact Mass |
373.211
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| CAS # |
80755-51-7
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| Related CAS # |
Bunazosin hydrochloride;52712-76-2
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| PubChem CID |
2472
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.221
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| Boiling Point |
620.6ºC at 760 mmHg
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| LogP |
2.652
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
494
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(CCC)N1CCCN(C2N=C3C(C=C(C(=C3)OC)OC)=C(N)N=2)CC1
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| InChi Key |
RHLJLALHBZGAFM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H27N5O3/c1-4-6-17(25)23-7-5-8-24(10-9-23)19-21-14-12-16(27-3)15(26-2)11-13(14)18(20)22-19/h11-12H,4-10H2,1-3H3,(H2,20,21,22)
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| Chemical Name |
1-[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-1,4-diazepan-1-yl]butan-1-one
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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 |
| 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 : ~100 mg/mL (~267.77 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 | 2.6777 mL | 13.3887 mL | 26.7773 mL | |
| 5 mM | 0.5355 mL | 2.6777 mL | 5.3555 mL | |
| 10 mM | 0.2678 mL | 1.3389 mL | 2.6777 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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