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> Norepinephrine [51-41-2]

Norepinephrine [51-41-2]

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Datasheet (EN)

Norepinephrine (Synonyms: Nor-Epirenan, L-Noradrenaline, Levophed, Levonoradrenaline, Levonor, Arterenol, ...)

Catalog No. T7044 Copy Product Info
Purity: 99.90%
Norepinephrine is an alkaloid neurotransmitter and an effective adrenergic receptor (AR) agonist that activates α1, α2, and β1 receptors. It is commonly used as a vasoactive agent for the treatment of shock and can also be used to induce cardiomyopathy models.

Norepinephrine

Copy Product Info
Synonyms Nor-Epirenan, L-Noradrenaline, Levophed, Levonoradrenaline, Levonor, Arterenol, Aktamin

Norepinephrine is an alkaloid neurotransmitter and an effective adrenergic receptor (AR) agonist that activates α1, α2, and β1 receptors. It is commonly used as a vasoactive agent for the treatment of shock and can also be used to induce cardiomyopathy models.

Norepinephrine
Cas No. 51-41-2
Other Forms of Norepinephrine:

Batch Information
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Purity:99.90%
Appearance:Solid
Color:White to Brown
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COA HPLC HNMR

Product Introduction
Norepinephrine AI Summary
Norepinephrine exhibits diverse bioactivity profiles, particularly in relation to adrenergic receptors. It shows significant affinity for Alpha-1A adrenergic receptors with selectivity over Alpha-1B and Alpha-1D receptors, demonstrating agonist potency in rat vas deferens and canine prostate tissues. It also binds strongly to the alpha-2 adrenergic receptor (Ki = 37 nM) in rat cortex and alpha-1 adrenergic receptor (Ki = 390 nM) in rat liver. This compound shows vasoconstrictor effects in animal models, such as the rat aorta and canine saphenous vein, and elicits notable cardiovascular responses, including reduced blood pressure and increased cardiac contractility in anesthetized rats. Additionally, Norepinephrine has exhibited agonistic activity at the human alpha2A, alpha2B, and alpha2C adrenergic receptors, along with the beta-3 adrenergic receptor with high intrinsic activity and a low EC50 value, demonstrating potency in stimulating cAMP production. The compound also impacts the dopamine receptor (D2) and shows varying affinities across other adrenergic, dopamine, and beta receptors in different tissue types and species. In terms of enzyme interactions, Norepinephrine inhibits Lamin A splicing, RECQ1, Tau fibril formation, TDP1, and several other enzymes with significant potency. It also shows inhibitory activity against human HDAC6 and interactions with various transport proteins like OCT2 and OATP1B1. While exhibiting substantial affinity for adrenergic receptors, Norepinephrine does not demonstrate notable liver toxicity and shows minimal side effects in terms of drug-induced liver injury. Overall, Norepinephrine presents a broad spectrum of bioactivities across multiple biological pathways, showcasing its potential as a multifaceted pharmacological agent..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Norepinephrine is an alkaloid neurotransmitter and an effective adrenergic receptor (AR) agonist that activates α1, α2, and β1 receptors. It is commonly used as a vasoactive agent for the treatment of shock and can also be used to induce cardiomyopathy models.
Targets&IC50
α1-adrenoceptor:330 nM (Ki), β1-adrenoceptor:740 nM (Ki), α2A-adrenoceptor:56 nM (Ki)
In vitro
METHODS: Adult hippocampal cells were treated with Norepinephrine (0.1-10 µM) for 10-13 days and the number of neurospheres was determined using classical neurosphere assay.
RESULTS: A significant increase in the number of neurospheres was obtained at 100 nm and in the presence of 1 µM Norepinephrine, and a twofold increase in the number of neurospheres was observed in the presence of 10 µM Norepinephrine. [1]
METHODS: Human pancreatic cancer cells BxPC-3 and Panc-1 were treated with Norepinephrine (10 µM) for 12-48 h. Cell viability was assayed by MTT Assay.
RESULTS: Norepinephrine treatment alone significantly enhanced the viability of PDAC cells. [2]
In vivo
METHODS: To test in vivo activity, Norepinephrine (0.2-2 mg/kga) was administered intraperitoneally to C57BL6/J mice fed a high-fat diet once daily for two weeks.
RESULTS: A subset of Norepinephrine-treated mice developed unexpected adverse events, including bladder dilatation and decreased renal perfusion due to renal discoloration. [3]
Disease Modeling Protocol
Sepsis-associated cardiomyopathy model
  • Modeling Mechanism：

    Norepinephrine (NE) and lipopolysaccharide (LPS) work synergistically to induce cardiomyopathy through SIRT3/HO-1 axis-mediated ferroptosis: ① NE alone has no significant cardiotoxicity, but it can exacerbate LPS-induced oxidative stress, increasing reactive oxygen species (ROS) and lipid peroxidation levels (4-HNE and MDA are elevated); ② It inhibits SIRT3 activity, relieves its inhibition of p300, promotes HO-1 acetylation and enhances stability, accelerates heme degradation and releases ferrous ions, and induces iron overload; ③ Iron overload and lipid peroxidation together induce cardiomyocyte ferroptosis, accompanied by myocardial hypertrophy and fibrosis, ultimately leading to heart failure.

  • Related Products：

    Norepinephrine (T7044)

  • Modeling Method：

    Experimental Subject：

    Mice, C57BL/6, 8–12 weeks old, Body weight 25–28 g

    Dosage and Administration Route：

    ① Core modelling (two-hit protocol):
    - First challenge: IntraperitoNorepinephrineal (i.p.) injection of LPS at 5 mg/kg, single dose;
    - Second challenge: SimultaNorepinephrineous LPS administration with subcutaNorepinephrineous implantation of osmotic pump; Norepinephrine at 2 µg/kg/min via continuous infusion for 9 days;
    ② Control treatment:
    - LPS-only group: intraperitoNorepinephrineal injection of 5 mg/kg LPS+osmotic pump infusion of physiological saliNorepinephrine;
    - Norepinephrine-only group: IntraperitoNorepinephrineal injection of physiological saliNorepinephrine+osmotic pump infusion of 2 µg/kg/min Norepinephrine;
    - Blank control: IntraperitoNorepinephrineal injection of saliNorepinephrine+osmotic pump infusion of saliNorepinephrine;
    ③ Intervention validation group (optional):
    - Ferroptosis inhibitor: Ferrostatin-1 (Fer-1), 2 mg/kg/day, intraperitoNorepinephrineal injection, administered concurrently with modelling;
    - SIRT3 activator: 2-APQC, 30 mg/kg, intraperitoNorepinephrineal injection, administered continuously throughout modelling period

    Dosing Frequency and Duration Model：

    First strike: single-dose administration;
    Secondary challenge: Continuous infusion for 9 days

  • Validation：

    1. Pathological Indicators: - Myocardial Injury: HE staining showed cardiomyocyte hypertrophy (cross-sectional area increased by more than 250), and Masson staining showed an increased proportion of interstitial fibrosis area (p<0.01); - Ferroplasmosis Characteristics: Transmission electron microscopy showed mitochondrial shrinkage, DHE staining showed increased ROS levels (fluorescence intensity more than 3 times that of the control group), and significantly increased ferrous ion content in tissues (OD value ≥0.4, p<0.001); 2. Molecular Indicators: - Ferroplasmosis Pathway: Western blot showed upregulated expression of HO-1 and 4-HNorepinephrine proteins and downregulated expression of SIRT3 (p<0.01); - Myocardial Markers: Serum troponin T (cTnT) and creatiNorepinephrine kinase isoenzyme (CK-MB) levels were significantly increased (p<0.001); 3. Functional Indicators: - Cardiac Function: Echocardiography showed that the left ventricular ejection fraction (EF%) decreased to below 60% (control group ≥80%, p<0.01); Survival status: The 9-day survival rate after modeling was more than 30% lower than that of the LPS group aloNorepinephrine (p<0.05).

*Precautions：

*References：Ma D,et,al. Norepinephrine exacerbates LPS-induced cardiomyopathy via SIRT3/HO-1 axis-mediated ferroptosis. Crit Care. 2025 Aug 13;29(1):354.

SynonymsNor-Epirenan, L-Noradrenaline, Levophed, Levonoradrenaline, Levonor, Arterenol, Aktamin
Chemical Properties
Molecular Weight169.18
FormulaC8H11NO3
Cas No.51-41-2
Smiles[C@@H](CN)(O)C1=CC(O)=C(O)C=C1
Relative Density.1.397 g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
0.1M HCl: 10 mg/mL (59.11 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 8.46 mg/mL (50.01 mM), Sonication and heating are recommended.
In Vivo Formulation
10% DMSO+90% Saline: 0.1 mg/mL (0.59 mM), Solution.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO/0.1M HCl
1mg5mg10mg50mg
1 mM5.9109 mL29.5543 mL59.1086 mL295.5432 mL
5 mM1.1822 mL5.9109 mL11.8217 mL59.1086 mL
10 mM0.5911 mL2.9554 mL5.9109 mL29.5543 mL
20 mM0.2955 mL1.4777 mL2.9554 mL14.7772 mL
50 mM0.1182 mL0.5911 mL1.1822 mL5.9109 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.