| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| Other Sizes |
| Targets |
IC50: α1 adrenoceptor and β1 adrenoceptor[1]
DL-Norepinephrine hydrochloride targets α1 and β1 adrenoceptors. As an adrenergic agonist, it stimulates these receptors, leading to vasoconstriction and increased blood pressure. It mimics the sympathomimetic actions of endogenous norepinephrine. By activating α1 receptors, it causes vasoconstriction in various vascular beds. By activating β1 receptors, it increases heart rate and cardiac contractility. |
|---|---|
| ln Vitro |
In vitro, DL-Norepinephrine hydrochloride acts as an adrenergic agonist, stimulating α1 and β1 adrenoceptors. Its activity is typically assessed by measuring its ability to stimulate calcium mobilization (for α1) or cAMP accumulation (for β1) in cells expressing these receptors. The compound's potency and efficacy as an adrenergic agonist can be determined and compared to reference agonists like norepinephrine or phenylephrine. It is used in studies of neurotransmitter signaling and cardiovascular regulation.
|
| ln Vivo |
In vivo, DL-Norepinephrine hydrochloride produces effects consistent with sympathomimetic stimulation, including vasoconstriction and increased blood pressure. It reduces subendocardial oxygen tension. It is widely used to study cardiovascular regulation, neurotransmitter signaling, and stress response mechanisms. The compound is a synthetic phenylethylamine that mimics the sympathomimetic actions of endogenous norepinephrine. It is classified as a dangerous good for transport.
|
| Enzyme Assay |
For non-cell-based receptor binding assays, DL-Norepinephrine hydrochloride can be evaluated using membrane preparations from tissues expressing α1 or β1 adrenoceptors. Radioligand binding displacement experiments are performed using suitable radiolabeled ligands such as [3H]-prazosin for α1 or [3H]-CGP-12177 for β1. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand at room temperature for 60-90 minutes. Bound radioligand is separated from free by rapid filtration through glass fiber filters. Non-specific binding is determined in the presence of excess unlabeled ligand. IC50 values are calculated from displacement curves.
|
| Cell Assay |
For in vitro cellular assays, cells expressing α1 or β1 adrenoceptors are cultured in appropriate media. For functional assays, intracellular calcium mobilization (for α1) or cAMP accumulation (for β1) is measured. Cells are treated with various concentrations of DL-Norepinephrine hydrochloride, and the signaling response is measured using fluorescent indicators or ELISA-based detection. EC50 values are calculated from dose-response curves. The compound's potency and efficacy as an adrenergic agonist can be determined.
|
| Animal Protocol |
For in vivo animal studies, DL-Norepinephrine hydrochloride can be administered to rodents via intravenous or intraperitoneal injection. In cardiovascular studies, blood pressure, heart rate, and cardiac output are monitored following compound administration. In models of stress response, neuroendocrine and behavioral responses are assessed. Dosing regimens vary depending on the specific model and desired exposure levels. The compound is classified as a dangerous good for transport.
|
| ADME/Pharmacokinetics |
DL-Norepinephrine hydrochloride has a molecular weight of 205.64 and a molecular formula of C8H11NO3·HCl. It is a synthetic phenylethylamine. The compound is classified as a dangerous good for transport and may be subject to additional shipping charges. It is for research use only and is not intended for human consumption.
|
| Toxicity/Toxicokinetics |
The toxicity profile of DL-Norepinephrine hydrochloride includes potential for hypertension, tachycardia, and cardiac arrhythmias at high doses due to its vasoconstrictor and positive chronotropic effects. The compound is classified as a dangerous good for transport. It is for research use only and is not intended for human consumption. Standard toxicological evaluation would include acute and repeated-dose toxicity studies, as well as assessment of cardiovascular function.
|
| References | |
| Additional Infomation |
Norepinephrine is a precursor to adrenaline secreted by the adrenal medulla and is a neurotransmitter widely distributed in the central and autonomic nervous systems. It is the primary neurotransmitter in most postganglionic sympathetic nerve fibers and in the diffuse projection system originating from the macula of the brain. It is also found in plants and is used as a sympathomimetic drug.
DL-Norepinephrine hydrochloride (CAS 55-27-6) is a synthetic phenylethylamine that mimics the sympathomimetic actions of endogenous norepinephrine. It is a neurotransmitter that targets α1 and β1 adrenoceptors. It reduces subendocardial oxygen tension. It is used in research to study cardiovascular regulation, neurotransmitter signaling, and stress response mechanisms. It is available for research purposes only. |
| Molecular Formula |
C8H12CLNO3
|
|---|---|
| Molecular Weight |
205.64
|
| Exact Mass |
205.05
|
| CAS # |
55-27-6
|
| Related CAS # |
DL-Norepinephrine-d6 hydrochloride;1219803-04-9;DL-Norepinephrine-d3 hydrochloride;1392208-07-9
|
| PubChem CID |
5923
|
| Appearance |
White to light brown solid powder
|
| Density |
1.397g/cm3
|
| Boiling Point |
442.6ºC at 760mmHg
|
| Melting Point |
140-144ºC (dec.)
|
| Flash Point |
221.5ºC
|
| LogP |
1.592
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
13
|
| Complexity |
142
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC(=C(C=C1C(CN)O)O)O.Cl
|
| InChi Key |
FQTFHMSZCSUVEU-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C8H11NO3.ClH/c9-4-8(12)5-1-2-6(10)7(11)3-5;/h1-3,8,10-12H,4,9H2;1H
|
| Chemical Name |
4-(2-amino-1-hydroxyethyl)benzene-1,2-diol;hydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
1M HCl: 100 mg/mL (486.29 mM)
DMSO: 50 mg/mL (243.14 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.89 mg/mL (4.33 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 8.9 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 0.89 mg/mL (4.33 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 8.9 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: ≥ 0.89 mg/mL (4.33 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 | 4.8629 mL | 24.3143 mL | 48.6287 mL | |
| 5 mM | 0.9726 mL | 4.8629 mL | 9.7257 mL | |
| 10 mM | 0.4863 mL | 2.4314 mL | 4.8629 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.
Link: https://clinicaltrials.gov/ct2/show/NCT06028256
Conditions:Anesthesia|Blood Pressure|NorepinephrineProducts are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
