| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Neldazosin targets the α1-adrenoceptor. It is a potent antagonist of this receptor. As a quinazoline-class α1-antagonist, it is structurally related to prazosin and doxazosin. By blocking α1-adrenoceptors, it inhibits smooth muscle contraction in vascular and prostate tissue, leading to vasodilation and improved urinary flow. Its reduced lipophilicity (LogP 0.581 vs. prazosin ~1.3) may minimize non-specific binding.
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| ln Vitro |
In vitro, Neldazosin acts as a potent α1-adrenoceptor antagonist. Its activity is typically assessed by measuring its ability to inhibit agonist-induced contraction of isolated smooth muscle preparations, such as rat aorta or prostate tissue. The compound's reduced lipophilicity (LogP 0.581) compared to prazosin (~1.3) and doxazosin (~2.5) may result in minimized non-specific binding, making it a candidate for in vitro assays.
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| ln Vivo |
In vivo, Neldazosin has been investigated preclinically for hypertension and benign prostatic hyperplasia (BPH). As an α1-adrenoceptor antagonist, it would be expected to lower blood pressure by causing vasodilation and to improve urinary flow by relaxing smooth muscle in the prostate and bladder neck. However, comprehensive in vivo efficacy data from published literature are limited.
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| Enzyme Assay |
For non-cell-based receptor binding assays, Neldazosin can be evaluated using membrane preparations from cells expressing human α1-adrenoceptor subtypes. Radioligand binding displacement experiments are performed using a suitable radiolabeled ligand such as [3H]-prazosin. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand. Bound radioligand is separated from free by rapid filtration through glass fiber filters. Non-specific binding is determined in the presence of excess unlabeled prazosin. Ki values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing human α1-adrenoceptor subtypes (α1A, α1B, α1D) are cultured in appropriate media. For functional assays, intracellular calcium mobilization is measured using fluorescent calcium indicators such as Fluo-4 AM. Cells are loaded with the dye and pre-incubated with various concentrations of Neldazosin. Receptor activation is stimulated by the addition of an α1-adrenoceptor agonist such as phenylephrine. Fluorescence intensity is measured using a fluorescence plate reader. The reduction in calcium signal compared to control wells indicates antagonist activity.
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| Animal Protocol |
For in vivo animal studies, Neldazosin can be administered to rodents via oral gavage or intraperitoneal injection. In models of hypertension (e.g., spontaneously hypertensive rats), blood pressure is monitored via tail-cuff or telemetry following compound administration. In models of benign prostatic hyperplasia, prostate weight and urinary function are assessed. Dosing regimens vary depending on the specific model and desired exposure levels. Blood and tissue samples may be collected for pharmacokinetic analysis.
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| ADME/Pharmacokinetics |
Neldazosin has a molecular weight of 375.43 g/mol and a molecular formula of C18H25N5O4. It has a LogP of 0.581, which is approximately 55% lower than prazosin (~1.3). The compound is a powder stable at -20°C for up to 3 years. It is supplied exclusively for laboratory research use and is not for human or veterinary applications.
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| Toxicity/Toxicokinetics |
The toxicity profile of Neldazosin has not been extensively reported. As an α1-adrenoceptor antagonist, potential adverse effects may include orthostatic hypotension, dizziness, and asthenia, which are common side effects of this class of compounds. The compound is for research use only and is not intended for human consumption. Standard toxicological evaluation would include acute and repeated-dose toxicity studies.
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| References |
[1]. Time course for blood pressure lowering of alpha blockers. Cochrane Database of Systematic Reviews 2012, Issue 9. Art. No.: CD010083. https://doi.org/10.1002/14651858.CD010083
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| Additional Infomation |
See also: Methyldopa (related).
Neldazosin is a research-grade α1-adrenoceptor antagonist of the quinazoline class. It is a prazosin derivative investigated preclinically for hypertension and benign prostatic hyperplasia (BPH). Its reduced lipophilicity (LogP 0.581) may minimize non-specific binding in in vitro assays. It is available for research purposes only and is not for human or veterinary use. |
| Molecular Formula |
C18H25N5O4
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|---|---|
| Molecular Weight |
375.42
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| Exact Mass |
375.191
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| CAS # |
109713-79-3
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| PubChem CID |
65908
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.313g/cm3
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| Boiling Point |
659.8ºC at 760mmHg
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| Flash Point |
352.8ºC
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| Vapour Pressure |
2.61E-18mmHg at 25°C
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| Index of Refraction |
1.629
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| LogP |
0.581
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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 |
5
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| Heavy Atom Count |
27
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| Complexity |
502
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| Defined Atom Stereocenter Count |
0
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| SMILES |
NC1C2C(=CC(OC)=C(OC)C=2)N=C(N2CCN(C(=O)CC(O)C)CC2)N=1
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| InChi Key |
IOSMPEJNAQZKJT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H25N5O4/c1-11(24)8-16(25)22-4-6-23(7-5-22)18-20-13-10-15(27-3)14(26-2)9-12(13)17(19)21-18/h9-11,24H,4-8H2,1-3H3,(H2,19,20,21)
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| Chemical Name |
1-[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-3-hydroxybutan-1-one
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| Synonyms |
Neldazosin; HRO 2/145; 109713-79-3; HRO-2/145; Neldazosin [INN]; Neldazosina; Neldazosine;
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.6637 mL | 13.3184 mL | 26.6368 mL | |
| 5 mM | 0.5327 mL | 2.6637 mL | 5.3274 mL | |
| 10 mM | 0.2664 mL | 1.3318 mL | 2.6637 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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