Cat. No.: HY-N2037

Higenamine

(Synonyms: Norcoclaurine; Demethyl-Coclaurine)

10 Cited Publications

Customer Review

Based on 10 publication(s) in Google Scholar

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.

Purity: 99.31%
CAS No.: 5843-65-2
Formula: C₁₆H₁₇NO₃
Molecular Weight:271.31

Storage:

4°C, sealed storage, away from moisture

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

Higenamine Chemical Structure

CAS No.: 5843-65-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (10)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

β adrenergic receptor

All MAP3K Isoforms :

All Adrenergic Receptor Isoforms :

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.

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.

Chemical Information

CAS No. 5843-65-2
Appearance Solid
Molecular Weight 271.31
Formula C₁₆H₁₇NO₃
Color White to off-white
SMILES

OC1=CC2=C(C(CC3=CC=C(O)C=C3)NCC2)C=C1O
Synonyms

Norcoclaurine; Demethyl-Coclaurine
Structure Classification
- Alkaloids
- Isoquinoline Alkaloids
- Phenols
- Polyphenols
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)

Publications (10)

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Journal Impact Factor

Cell

GRK-biased adrenergic agonists for the treatment of type 2 diabetes and obesity. [Abstract]

2025 Sep 18;188(19):5142-5156.e23. PMID: 40555230
Food Sci Hum Wellness

2025.
Arch Toxicol

Quantitative in vitro-to-in vivo extrapolation of human adrenergic and trace amine-associated receptor 1 potencies of pre-workout supplement ingredients using physiologically based kinetic modelling-based reverse dosimetry. [Abstract]

2025 May;99(5):1999-2021. PMID: 40178592
Ind Crops Prod

2025 Dec 2;238:122414.
Nutrients

In Vitro Activation of Human Adrenergic Receptors and Trace Amine-Associated Receptor 1 by Phenethylamine Analogues Present in Food Supplements. [Abstract]

2024 May 22;16(11):1567. PMID: 38892500
Eur J Pharmacol

Phenethylamines in pre-workout supplements alter arterial pressure, heart rate, and body temperature in rats. [Abstract]

2026 Jun 10:1026:178966. PMID: 42128191
Toxicology

In vitro inhibition of monoamine transport by amphetamine-like pre-workout supplement ingredients. [Abstract]

2026 Mar 6:154442. PMID: 41796714
J Inflamm Res

Shenfu Injection Mediated NLRP3/Caspase 1 Through (R)-Norcoclaurinee Alleviates Sepsis-Induced Cognitive Dysfunction. [Abstract]

2024 Oct 14:17:7295-7310. PMID: 39429846
Cardiovasc Toxicol

Potential Cardiovascular Risks of Phenethylamine Analogues in Food Supplements: Evidence from Vasocontraction of Rat Artery Segments. [Abstract]

2026 Apr 4;26(4):36. PMID: 41934574
J Pharm Biomed Anal

Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]

2021 Feb 20:195:113870. PMID: 33453569

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)

H₂O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.6858 mL

18.4291 mL

36.8582 mL

5 mM

0.7372 mL

3.6858 mL

7.3716 mL

10 mM

0.3686 mL

1.8429 mL

3.6858 mL

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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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In Vivo:

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

Stock Solution Working Solution

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.

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Fang Y, et al. Discovery of higenamine as a potent, selective and cellular active natural LSD1 inhibitor for MLL-rearranged leukemia therapy. Bioorg Chem. 2021 Apr;109:104723. [Content Brief]

[2]. Ha YM, et al. Higenamine reduces HMGB1 during hypoxia-induced brain injury by induction of heme oxygenase-1 through PI3K/Akt/Nrf-2 signal pathways. Apoptosis. 2012 May;17(5):463-74. [Content Brief]

[3]. Zhu X, et al. Higenamine mitigates interleukin-1β-induced human nucleus pulposus cell apoptosis by ROS-mediated PI3K/Akt signaling. Mol Cell Biochem. 2021 Nov;476(11):3889-3897. [Content Brief]

[4]. Deng T, et al. Higenamine Improves Cardiac and Renal Fibrosis in Rats With Cardiorenal Syndrome via ASK1 Signaling Pathway. J Cardiovasc Pharmacol. 2020 Jun;75(6):535-544. [Content Brief]

[5]. Erasto, Paul et al. Evaluation of Antimycobacterial Activity of Higenamine Using Galleria mellonella as an In Vivo Infection Model. Natural products and bioprospecting vol. 8,1 (2018): 63-69. [Content Brief]

[6]. Dong, Hui et al. Higenamine Promotes Osteogenesis Via IQGAP1/SMAD4 Signaling Pathway and Prevents Age- and Estrogen-Dependent Bone Loss in Mice. Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research vol. 38,5 (2023): 775-791. [Content Brief]

[7]. Wu MP, et al. Higenamine protects ischemia/reperfusion induced cardiac injury and myocyte apoptosis through activation of β2-AR/PI3K/AKT signaling pathway. Pharmacol Res. 2016 Feb;104:115-23. [Content Brief]

[8]. Lee SR, et al. Acute oral intake of a higenamine-based dietary supplement increases circulating free fatty acidsand energy expenditure in human subjects. Lipids Health Dis. 2013 Oct 21;12:148. [Content Brief]

[9]. Wen J, et al. Role of Higenamine in Heart Diseases: A Mini-Review. Front Pharmacol. 2022 Jan 10;12:798495. [Content Brief]

[10]. Chen DT, et al. Pharmacological effects of higenamine based on signalling pathways and mechanism of action. Front Pharmacol. 2022 Sep 15;13:981048. [Content Brief]

[11]. Romeo I, et al. The Antioxidant Capability of Higenamine: Insights from Theory. Antioxidants (Basel). 2020 Apr 25;9(5):358. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Apoptosis Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

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Protein Tyrosine Kinase Compound Library

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RO5 Drug-like Natural Product Library

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Publications Citing Use of MedChemExpress (MCE) Higenamine

All MAP3K Isoforms

All Adrenergic Receptor Isoforms

Biological Activity

Chemical Information

Publications (10)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Higenamine Related Classifications

Cat. No.: HY-N2037