2. MAPK/ERK Pathway GPCR/G Protein Neuronal Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. MAP3K MDM-2/p53 Adrenergic Receptor ROS Kinase Apoptosis
  4. Higenamine

Higenamine  (Synonyms: Norcoclaurine; Demethyl-Coclaurine)

Cat. No.: HY-N2037 Purity: 98.91%
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Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases.

For research use only. We do not sell to patients.

Higenamine Chemical Structure

Higenamine Chemical Structure

CAS No. : 5843-65-2

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10 mg USD 80 In-stock
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Based on 3 publication(s) in Google Scholar

Other Forms of Higenamine:

Higenamine Related Antibodies

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α adrenergic receptor β adrenergic receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases[1][2][3][4][5][6][7][8][9][10][11].

IC50 & Target

β adrenergic receptor

 

In Vitro

Higenamine (3-100 μM; 72 h) can inhibit the differentiation of MV4-11 and MOLM-13 cells by inhibiting the activity of LSD1[1].
Higenamine (1-100μM; 8 h) can enhance the activity of HO-1 in C6 cells and protect brain cells from cell hypoxia damage [2].
Higenamine (10-50 μM; 8 h) can inhibit apoptosis in C6 cells[2].
Higenamine (10-40 μM; 24 h) can inhibit the production of IL-1β-induced ROS and activate the ROS-mediated PI3K/Akt signaling pathway, which has anti-apoptotic activity in HNPCs[3].
Higenamine (0.08-250 μM; 0.5-24 h) promotes phosphorylation of SMAD2/3 in a time- and dose-dependent manner in BMSCs[6].
Higenamine (0-120 μM, 24 h) reverses H2O2 (250 μM, 24 h) induced cell death and apoptosis in neonatal rat ventricular myocytes (NRVMs)[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Higenamine Related Antibodies

Western Blot Analysis[1]

Cell Line: MV4-11, MOLM-13
Concentration: 3 μM, 10 μM, 30 μM, 100 μM
Incubation Time: 72 h
Result: Could up-regulate the expression levels of LSD1 substrate H3K4me1 and H3K4me2 in a dose-dependent manner, but did not affect the expression levels of H3K4me3, H3 and LSD1.
Promoted P53 expression in a dose-dependent manner.

Western Blot Analysis[2]

Cell Line: C6
Concentration: 1 μM, 5μM, 10 μM, 50 μM,100 μM
Incubation Time: 8 h
Result: Increased HO-1 expression in a concentration-dependent manner under hypoxia and normoxia conditions.

Real Time qPCR[1]

Cell Line: MV4-11, MOLM-13
Concentration: 3 μM, 10 μM, 30 μM, 100 μM
Incubation Time: 72 h
Result: Significantly down-regulated the expression levels of HoxA9 and Meis1 in leukemia cells in a dose-dependent manner.

Apoptosis Analysis[7]

Cell Line: NRVMs
Concentration: 0-120 μM
Incubation Time: 24 h
Result: Dose dependently attenuated H2O2-stimulated early and late apoptosis of NRVMs.
In Vivo

Higenamine hydrochloride (10 mg/kg; Intraperitoneal injection; Single dose) can significantly reduce the inflammation and infarct size of cerebral ischemic injury caused by middle cerebral artery occlusion (MCAO) in Sprague-Dawley rats[2].
Higenamine hydrochloride (0.5-4.5 mg/kg; Single dose) improves cardiac and renal function in rats with cardio-renal syndrome (CRS) and alleviates cardiac and renal fibrosis by targeting ASK1/MAPK (ERK, P38)/NF-kB signaling pathway in Sprague-Dawley rats[4].
Higenamine hydrochloride (20 mg/kg-30 mg/kg; Intraperitoneal injection; Once daily for 60 days) promotes bone formation and prevents accelerated bone loss in SAMP6 mice[6].
Higenamine (10 mg/kg, i.p., 2 h prior to the surgery) protects against I/R-induced myocardial infarction in mice bearing ischemia/reperfusion injury[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Spontaneous osteoporosis SAMP6 mice model[6]
Dosage: 10 mg/kg, 20 mg/kg
Administration: Intraperitoneal injection (i.p.);Once daily for 60 days
Result: Significantly increased the expression of P1NP and OCN (P1NP and OCN are markers of bone formation).
Animal Model: Mice bearing ischemia/reperfusion injury[7]
Dosage: 10 mg/kg
Administration: i.p., 2 h prior to the surgery
Result: Decreased the myocardial infarct areas (MI) and increased myocyte survival in mice bearing ischemia/reperfusion injury.
Clinical Trial
Molecular Weight

271.31

Formula

C16H17NO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC1=CC2=C(C(CC3=CC=C(O)C=C3)NCC2)C=C1O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (368.58 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6858 mL 18.4291 mL 36.8582 mL
5 mM 0.7372 mL 3.6858 mL 7.3716 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.91%

SDS (393 KB)

COA (248 KB) HNMR (252 KB) LCMS (87 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6858 mL 18.4291 mL 36.8582 mL 92.1455 mL
5 mM 0.7372 mL 3.6858 mL 7.3716 mL 18.4291 mL
10 mM 0.3686 mL 1.8429 mL 3.6858 mL 9.2146 mL
15 mM 0.2457 mL 1.2286 mL 2.4572 mL 6.1430 mL
20 mM 0.1843 mL 0.9215 mL 1.8429 mL 4.6073 mL
25 mM 0.1474 mL 0.7372 mL 1.4743 mL 3.6858 mL
30 mM 0.1229 mL 0.6143 mL 1.2286 mL 3.0715 mL
40 mM 0.0921 mL 0.4607 mL 0.9215 mL 2.3036 mL
50 mM 0.0737 mL 0.3686 mL 0.7372 mL 1.8429 mL
60 mM 0.0614 mL 0.3072 mL 0.6143 mL 1.5358 mL
80 mM 0.0461 mL 0.2304 mL 0.4607 mL 1.1518 mL
100 mM 0.0369 mL 0.1843 mL 0.3686 mL 0.9215 mL
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Higenamine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Higenamine5843-65-2Norcoclaurine Demethyl-CoclaurineMAP3KMDM-2/p53Adrenergic ReceptorROS KinaseApoptosisMAP kinase kinase kinase, MEKK, MAPKKKBeta Receptorβ2-ARheart failuremyocyteischemia/reperfusionmyocardial infarctionosteoporosisLeukemiaMV4-11MOLM-13strokeCRSC6HNPCsBMSCsInhibitorinhibitorinhibit

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