| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
|
||
| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Norepinephrine hydrochloride acts as an agonist at α1, α2, and β1 adrenergic receptors. It has high affinity for α1 receptors, leading to vasoconstriction and increased peripheral vascular resistance. It also activates β1 receptors in the heart, increasing cardiac contractility and heart rate. It has relatively low affinity for β2 receptors. The compound is a catecholamine and is synthesized from dopamine by dopamine β-hydroxylase.
|
|---|---|
| ln Vitro |
While β2-norrepinephrine is absorbed, norepinephrine hydrochloride (Levarterenol; L-norepinephrine) is usually regarded as a β1-subtype intermittent agonist. At significant concentrations, norepinephrine hydrochloride (NE) hydrochloride also directly affects β2-primergic absorption [2]. From newborn wild-type C57BL/6J mice, adipocytes were isolated and cultured from the inguinal fat pad (iWA) or the intershoulder fat pad (BA). cAMP production in response to co-treatment with norepinephrine hydrochloride (NE, 10 μM) with or without CGP (10 nM) was first measured in order to investigate the impact of activating AT2 on β-initiergic signaling. Sex activates the UCP1 protein and increases heat production. Norepinephrine Hydrochloride (NE) increases cAMP as expected in iWA; CGP does not change the effect. Norepinephrine Hydrochloride (NE) is also known to induce lipogenesis and requires released nutrients to function. Following therapy, CREB phosphorylation at Ser133 rose and was considerably reduced by concurrent CGP treatment [3].
In vitro, norepinephrine hydrochloride activates adrenergic receptors in various cell systems. It stimulates contraction of vascular smooth muscle cells via α1 receptor activation. In cardiac myocytes, it increases contractility via β1 receptor activation. It can be used to study adrenergic signaling pathways, including cAMP and IP3/DAG cascades. It also modulates neurotransmitter release in neuronal cultures. |
| ln Vivo |
In vivo, norepinephrine hydrochloride causes vasoconstriction, increased blood pressure, and increased cardiac output. It is used as a vasopressor agent to treat septic shock and other forms of hypotension. It increases systemic vascular resistance and venous return. It also has effects on metabolism, including glycogenolysis and lipolysis. In the CNS, it plays a role in arousal, attention, and mood regulation.
|
| Enzyme Assay |
For non-cellular enzyme/receptor binding assays, radioligand binding assays are used to assess affinity for adrenergic receptor subtypes. Competitive binding experiments using [3H]prazosin (α1), [3H]rauwolscine (α2), or [3H]CGP-12177 (β) are performed. Ki values are determined. Functional assays such as cAMP accumulation or GTPγS binding can be used to assess agonist activity at β and α2 receptors, respectively.
|
| Cell Assay |
For in vitro cell-based assays, cells expressing adrenergic receptors are cultured and treated with norepinephrine hydrochloride. Receptor activation is measured by cAMP accumulation (for β receptors) or intracellular calcium mobilization (for α1 receptors). Cell proliferation, viability, and signaling pathway activation (e.g., MAPK, PI3K) can be assessed using standard assays.
|
| Animal Protocol |
For in vivo studies, norepinephrine hydrochloride is administered to animal models via intravenous infusion. Cardiovascular parameters such as blood pressure, heart rate, and peripheral vascular resistance are measured. It is used in models of septic shock, hypotension, and cardiac arrest. Dosing and route of administration depend on the specific experimental model and clinical indication.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties include solubility in water and saline. The molecular weight is C8H11NO3·HCl. It is a catecholamine and is rapidly metabolized by monoamine oxidase (MAO) and catechol-O-methyltransferase (COMT). It has a short half-life in the circulation. Storage is typically at -20°C, protected from light. It is a solid and should be handled with standard laboratory precautions.
|
| Toxicity/Toxicokinetics |
Toxicological data for norepinephrine hydrochloride is well-established from its clinical use. At high doses, it can cause severe hypertension, arrhythmias, ischemia, and tissue necrosis due to extravasation. It can also cause anxiety, headaches, and respiratory distress. It is not for human use in research settings without appropriate approval.
|
| 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.
Norepinephrine hydrochloride is a potent vasopressor and adrenergic agonist. It is used clinically to treat hypotension and shock. It acts primarily on α1 receptors to cause vasoconstriction and increase blood pressure. It also activates β1 receptors in the heart. It is a key neurotransmitter in the sympathetic nervous system and plays important roles in stress responses, attention, and mood regulation. |
| Molecular Formula |
C₈H₁₂CLNO₃
|
|---|---|
| Molecular Weight |
205.63878
|
| Exact Mass |
205.05
|
| CAS # |
329-56-6
|
| Related CAS # |
Norepinephrine;51-41-2;Norepinephrine bitartrate monohydrate;108341-18-0;Norepinephrine tartrate;51-40-1
|
| PubChem CID |
11672905
|
| Appearance |
Off-white to yellow solid powder
|
| Density |
1.397g/cm3
|
| Boiling Point |
442.6ºC at 760mmHg
|
| Melting Point |
-150ºC (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 |
1
|
| SMILES |
C1=CC(=C(C=C1[C@H](CN)O)O)O.Cl
|
| InChi Key |
FQTFHMSZCSUVEU-QRPNPIFTSA-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,4,9H21H/t8-/m0./s1
|
| Chemical Name |
(R)-4-(2-amino-1-hydroxyethyl)benzene-1,2-diol hydrochloride
|
| Synonyms |
Levarterenol hydrochloride L-Noradrenaline hydrochloride L-Norepinephrine HCl L-Arterenol hydrochloride L-Arterenol HCl Aktamin 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) |
H2O : ~250 mg/mL (~1215.72 mM)
DMSO : ~44 mg/mL (~213.97 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.11 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 20.8 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: ≥ 2.08 mg/mL (10.11 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 20.8 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: ≥ 2.08 mg/mL (10.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 33.33 mg/mL (162.08 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| 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.