Higenamine hydrochloride
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.
For research use only. We do not sell to patients.
- Purity: 99.34%
- CAS No.: 11041-94-4
- Formula: C16H18ClNO3
- Molecular Weight:307.77
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Storage:
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)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Higenamine hydrochloride
More- Cell. 2025 Sep 18;188(19):5142-5156.e23. [Abstract]
- Food Sci Hum Wellness. 2025.
- Arch Toxicol. 2025 May;99(5):1999-2021. [Abstract]
- Ind Crops Prod. 2025 Dec 2;238:122414.
- Nutrients. 2024 May 22;16(11):1567. [Abstract]
- Eur J Pharmacol. 2026 Jun 10:1026:178966. [Abstract]
- Toxicology. 2026 Mar 6:154442. [Abstract]
- J Inflamm Res. 2024 Oct 14:17:7295-7310. [Abstract]
- Cardiovasc Toxicol. 2026 Apr 4;26(4):36. [Abstract]
- J Pharm Biomed Anal. 2021 Feb 20:195:113870. [Abstract]
All MAP3K Isoforms
More
Biological Activity
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β adrenergic receptor |
ASK1 |
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.
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Cell Line:MV4-11, MOLM-13
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Concentration:3 μM, 10 μM, 30 μM, 100 μM
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Incubation Time:72 h
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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.
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Cell Line:C6
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Concentration:1 μM, 5μM, 10 μM, 50 μM,100 μM
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Incubation Time:8 h
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Result:Increased HO-1 expression in a concentration-dependent manner under hypoxia and normoxia conditions.
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Cell Line:MV4-11, MOLM-13
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Concentration:3 μM, 10 μM, 30 μM, 100 μM
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Incubation Time:72 h
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Result:Significantly down-regulated the expression levels of HoxA9 and Meis1 in leukemia cells in a dose-dependent manner.
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.
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Animal Model:Spontaneous osteoporosis SAMP6 mice model[6]
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Dosage:10 mg/kg, 20 mg/kg
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Administration:Intraperitoneal injection (i.p.);Once daily for 60 days
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Result:Significantly increased the expression of P1NP and OCN (P1NP and OCN are markers of bone formation).
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 11041-94-4
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Appearance Solid
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Molecular Weight 307.77
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Formula C16H18ClNO3
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Color White to off-white
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SMILES
OC1=CC2=C(C(CC3=CC=C(O)C=C3)NCC2)C=C1O.Cl
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Synonyms
Norcoclaurine hydrochloride
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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
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Most Recent
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Cell
2025 Sep 18;188(19):5142-5156.e23. PMID: 40555230 -
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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 -
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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
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (324.92 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (282 KB)
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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)
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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]
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, 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.
| 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.
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