| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Phentolamine Analogue 1 targets adrenergic receptors, specifically alpha-adrenergic receptors. Like phentolamine, it is a nonselective alpha-adrenergic antagonist that blocks both alpha-1 and alpha-2 adrenergic receptors. By blocking these receptors, the compound inhibits the effects of endogenous catecholamines (norepinephrine and epinephrine) on vascular smooth muscle and other tissues. This mechanism is relevant for studying cardiovascular function and the sympathetic nervous system.
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| ln Vitro |
The analogue of phentolamine is pentolamine analogue 1 (3h) [1].
In vitro, Phentolamine Analogue 1 has been studied for its ability to bind to and inhibit alpha-adrenergic receptors. The compound's affinity and selectivity for different adrenergic receptor subtypes are characterized in radioligand binding assays and functional assays. These studies help to understand the structure-activity relationships of phentolamine analogues and to develop improved alpha-adrenergic antagonists. |
| ln Vivo |
In vivo, Phentolamine Analogue 1 is used in animal models to study the physiological effects of alpha-adrenergic receptor blockade. The compound's effects on blood pressure, heart rate, and vascular tone are evaluated in vivo. These studies contribute to the understanding of adrenergic receptor physiology and the development of new therapeutic agents for cardiovascular and other diseases.
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| Enzyme Assay |
The in vitro receptor binding assay for Phentolamine Analogue 1 measures its affinity for alpha-adrenergic receptors. Radioligand binding assays are performed using membrane preparations from tissues expressing alpha-1 and alpha-2 adrenergic receptors, with radiolabeled phentolamine or other alpha-adrenergic ligands. The compound's ability to displace the radioligand is measured, and IC50 and Ki values are calculated. Selectivity is assessed by testing against other receptor types.
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| Cell Assay |
In vitro cellular studies are conducted using cell lines expressing adrenergic receptors. Cells are treated with Phentolamine Analogue 1 at various concentrations, and downstream signaling is measured (e.g., cAMP, calcium mobilization, or MAPK activation). Functional assays evaluate the compound's ability to inhibit agonist-induced responses. Cell viability and cytotoxicity are also assessed. These studies characterize the compound's pharmacological profile and mechanism of action.
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| Animal Protocol |
In vivo animal experiments are performed using rodent models to study cardiovascular effects. Animals are administered Phentolamine Analogue 1 via intravenous, intraperitoneal, or oral administration at various doses. Blood pressure, heart rate, and other cardiovascular parameters are monitored. The compound's effects on vascular tone and sympathetic nervous system function are evaluated. These studies help to characterize the in vivo pharmacology of the compound.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Phentolamine Analogue 1 include solubility in DMSO (45 mg/mL). The compound has a molecular weight of 281.35 g/mol, molecular formula C17H19N3O, and density of 1.18 g/cm³ (predicted). Storage at -20°C for powder is recommended. The compound should be protected from light and moisture. It appears as a solid at room temperature.
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| Toxicity/Toxicokinetics |
Toxicological data for Phentolamine Analogue 1 are limited to preclinical studies. The compound is for research use only and not intended for human therapeutic applications. No significant toxicity has been reported at effective doses in animal studies. Standard safety precautions should be followed when handling the compound. Long-term toxicity and carcinogenicity studies have not been conducted.
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| References | |
| Additional Infomation |
Phentolamine Analogue 1 is an analogue of phentolamine, a nonselective alpha-adrenergic antagonist. The compound is used in research to study adrenergic receptor signaling and to develop improved alpha-adrenergic antagonists. It has the molecular formula C17H19N3O and molecular weight of 281.35 g/mol. The compound is supplied as a powder and should be stored under recommended conditions. It is not for human use and is intended for research purposes only.
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| Molecular Formula |
C17H19N3O
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| Molecular Weight |
281.352263689041
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| Exact Mass |
281.15
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| Elemental Analysis |
C, 72.57; H, 6.81; N, 14.94; O, 5.69
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| CAS # |
47142-51-8
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| PubChem CID |
66147
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
355
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=C(C=C1)N(CC2=NCCN2)C3=CC=C(C=C3)O.Cl
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| InChi Key |
JZYAMURVBSVJTK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H19N3O.ClH/c1-13-2-4-14(5-3-13)20(12-17-18-10-11-19-17)15-6-8-16(21)9-7-15;/h2-9,21H,10-12H2,1H3,(H,18,19);1H
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| Chemical Name |
4-[N-(4,5-dihydro-1H-imidazol-2-ylmethyl)-4-methylanilino]phenol;hydrochloride
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| Synonyms |
Phentolamine Analogue 1; LUN42518; LUN-42518; LUN 42518;
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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 | 3.5543 mL | 17.7715 mL | 35.5429 mL | |
| 5 mM | 0.7109 mL | 3.5543 mL | 7.1086 mL | |
| 10 mM | 0.3554 mL | 1.7771 mL | 3.5543 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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