Art. -Nr.: HY-N2037A

Higenamine hydrochloride

(Synonyms: Norcoclaurine hydrochloride)

10 Cited Publications

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Based on 10 publication(s) in Google Scholar

Higenamine hydrochloride is a selective LSD1 inhibitor (IC₅₀=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine (Norcoclaurine) can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine hydrochloride protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine hydrochloride can be used to study cancer, inflammation, cardiorenal syndrome and other diseases.

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Reinheit: 99.34%
CAS. Nr.: 11041-94-4
Formel: C₁₆H₁₈ClNO₃
Molecular Weight:307.77

Speicherung:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)

Higenamine hydrochloride Chemical Structure

CAS. Nr.: 11041-94-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (10)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

β adrenergic receptor

ASK1

Alle MAP3K Isoform-spezifische Produkte anzeigen :

In Vitro

Higenamine hydrochloride (3-100 μM; 72 h) can inhibit the differentiation of MV4-11 and MOLM-13 cells by inhibiting the activity of LSD1^[1].
Higenamine hydrochloride (1-100μM; 8 h) can enhance the activity of HO-1 in C6 cells and protect brain cells from cell hypoxia damage ^[2].
Higenamine hydrochloride (10-50 μM; 8 h) can inhibit apoptosis in C6 cells^[2].
Higenamine hydrochloride (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 hydrochloride (0.08-250 μM; 0.5-24 h) promotes phosphorylation of SMAD2/3 in a time- and dose-dependent manner in BMSCs^[6].

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.

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].

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).

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 11041-94-4
Appearance Solid
Molecular Weight 307.77
Formel C₁₆H₁₈ClNO₃
Color White to off-white
SMILES

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

Norcoclaurine hydrochloride
Structure Classification
- Alkaloids
- Isoquinoline Alkaloids
- Phenols
- Polyphenols
Initial Source
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)

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
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
Food Sci Hum Wellness

2025.
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
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
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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (324.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 10 mg/mL (32.49 mM; Need ultrasonic)

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

3.2492 mL

16.2459 mL

32.4918 mL

5 mM

0.6498 mL

3.2492 mL

6.4984 mL

10 mM

0.3249 mL

1.6246 mL

3.2492 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, 2 years; -20°C, 1 year (sealed storage, away from moisture and light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: ≥ 2.08 mg/mL (6.76 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.76 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: PBS

Solubility: 100 mg/mL (324.92 mM); Clear solution; Need ultrasonic

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 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)
- Korean - KR (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)

Verweise

[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]

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
H₂O / DMSO	1 mM	3.2492 mL	16.2459 mL	32.4918 mL	81.2295 mL
	5 mM	0.6498 mL	3.2492 mL	6.4984 mL	16.2459 mL
	10 mM	0.3249 mL	1.6246 mL	3.2492 mL	8.1229 mL
	15 mM	0.2166 mL	1.0831 mL	2.1661 mL	5.4153 mL
	20 mM	0.1625 mL	0.8123 mL	1.6246 mL	4.0615 mL
	25 mM	0.1300 mL	0.6498 mL	1.2997 mL	3.2492 mL
	30 mM	0.1083 mL	0.5415 mL	1.0831 mL	2.7076 mL
DMSO	40 mM	0.0812 mL	0.4061 mL	0.8123 mL	2.0307 mL
	50 mM	0.0650 mL	0.3249 mL	0.6498 mL	1.6246 mL
	60 mM	0.0542 mL	0.2708 mL	0.5415 mL	1.3538 mL
	80 mM	0.0406 mL	0.2031 mL	0.4061 mL	1.0154 mL
	100 mM	0.0325 mL	0.1625 mL	0.3249 mL	0.8123 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Higenamine hydrochloride

10 Cited Publications

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Higenamine hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Higenamine hydrochloride

Alle MAP3K Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (10)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Higenamine hydrochloride Related Classifications

HY-N2037A Related Classifications