| Size | Price | Stock | Qty |
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| Targets |
Butoxamine's primary target is the β2-adrenergic receptor. It acts as a selective antagonist, meaning it binds to and blocks the receptor without activating it. This prevents the binding of endogenous agonists like epinephrine and norepinephrine, thereby inhibiting β2-receptor-mediated signaling. This selectivity for β2 over β1 receptors makes it a valuable tool for studying the distinct physiological roles of the β2 receptor subtype.
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| ln Vitro |
Butoxamine hydrochloride is used in vitro to study the function of β2-adrenergic receptors. In cell-based assays, it is used to block β2 receptors to determine the contribution of this specific receptor subtype to a given cellular response. For example, it can be used to inhibit the effects of β2 agonists on smooth muscle relaxation or metabolic pathways. It is also used in tissue bath experiments to characterize receptor pharmacology in isolated tissues.
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| ln Vivo |
In ethanol-anesthetized, water-diuretic conditions, butasamine hydrochloride (25 μg/kg/min, 50 μg/kg/min, 100 μg/kg/min, 15 minutes; intravenously) raises urine output levels [1].
In vivo, Butoxamine hydrochloride is used to study the physiological roles of β2 receptors. It has been shown to inhibit the decrease in urine output in rats anesthetized with ethanol during water diuresis. This demonstrates its ability to block β2-mediated effects in a whole-animal model. It is also used to study the role of β2 receptors in the cardiovascular system and other physiological processes. |
| Enzyme Assay |
The in vitro activity of Butoxamine hydrochloride is determined in radioligand binding assays. In these cell-free experiments, the β2-adrenergic receptor (from animal or human tissues) is incubated with a radiolabeled ligand (e.g., [3H]-CGP-12177) and varying concentrations of Butoxamine. The amount of bound radioligand is measured, and the concentration of Butoxamine that displaces 50% of the specific binding (Ki or IC50) is calculated. This provides a measure of its receptor binding affinity.
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| Cell Assay |
In cell-based assays, Butoxamine hydrochloride is used to block β2 receptors. Cells expressing the β2 receptor are pre-incubated with Butoxamine before stimulation with a β2 agonist, such as salbutamol or isoproterenol. The effect of the agonist on a downstream signaling pathway, such as cAMP accumulation, is then measured. Butoxamine's ability to inhibit this response confirms its antagonist activity and allows researchers to isolate the β2-mediated component of the signaling.
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| Animal Protocol |
The in vivo activity of Butoxamine hydrochloride is evaluated in animal models. In a typical protocol, rats are anesthetized with ethanol and subjected to water diuresis. The animals are then treated with Butoxamine hydrochloride via intravenous infusion at rates such as 25, 50, or 100 μg/kg/min for 15 minutes. The effect on urine output is then measured. This model is used to study the role of β2 receptors in renal function.
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| ADME/Pharmacokinetics |
Butoxamine hydrochloride has a molecular weight of 303.82 and a molecular formula of C15H25NO3•HCl. It is typically supplied as a powder for research use. For in vivo studies, it is formulated in a suitable vehicle (e.g., saline) and administered via injection. Pharmacokinetic data is not typically a focus for this compound, as it is used primarily as a pharmacological tool rather than a therapeutic agent.
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| Toxicity/Toxicokinetics |
As a research tool, Butoxamine hydrochloride is generally considered safe when handled with standard laboratory precautions. Its toxicity profile is not extensively documented in the provided sources, as it is not a therapeutic drug. However, like all β-blockers, it has the potential to affect cardiovascular and respiratory function, and appropriate safety measures should be taken when handling and using the compound, especially in vivo.
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| References | |
| Additional Infomation |
A β2-selective adrenergic antagonist. It is primarily used in animal and tissue experiments to characterize β2-adrenergic receptors.
Butoxamine hydrochloride is a selective β2-adrenergic receptor antagonist. It is a research tool used to study the physiological and pharmacological roles of β2 receptors. It is also known as Butaxamine hydrochloride. It is not a therapeutic drug but is essential for dissecting the distinct functions of β-adrenergic receptor subtypes in various experimental systems. |
| Molecular Formula |
C15H26CLNO3
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|---|---|
| Molecular Weight |
303.82484
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| Exact Mass |
303.16
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| Elemental Analysis |
C, 59.30; H, 8.63; Cl, 11.67; N, 4.61; O, 15.80
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| CAS # |
5696-15-1
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| Related CAS # |
Butaxamine;2922-20-5
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| PubChem CID |
18026
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| Appearance |
White to off-white solid powder
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| Boiling Point |
391ºC at 760 mmHg
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| Flash Point |
190.3ºC
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| LogP |
3.706
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
19
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| Complexity |
265
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
TWUSDDMONZULSC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H25NO3/c1-10(16-15(2,3)4)14(17)12-9-11(18-5)7-8-13(12)19-6/h7-10,14,16-17H,1-6H3
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| Chemical Name |
2-(tert-butylamino)-1-(2,5-dimethoxyphenyl)propan-1-ol
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| Synonyms |
NSC-106565 HCl; NSC 106565 HCl; Butoxamine HCl; NSC 106565 HCl; NSC-106,565; NSC106,565 HCl; Butoxamine hydrochloride
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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 : ~100 mg/mL (~329.14 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.23 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 (8.23 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (8.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2914 mL | 16.4571 mL | 32.9142 mL | |
| 5 mM | 0.6583 mL | 3.2914 mL | 6.5828 mL | |
| 10 mM | 0.3291 mL | 1.6457 mL | 3.2914 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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