2. Apoptosis Protein Tyrosine Kinase/RTK
  3. MDM-2/p53 ROS Kinase Apoptosis
  4. Higenamine hydrochloride

Higenamine hydrochloride  (Synonyms: Norcoclaurine hydrochloride)

Cat. No.: HY-N2037A Purity: 99.68%
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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.

Higenamine hydrochloride Chemical Structure

Higenamine hydrochloride Chemical Structure

CAS No. : 11041-94-4

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of Higenamine hydrochloride:

Higenamine hydrochloride Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Higenamine hydrochloride

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3][4][5][6].

IC50 & Target

β adrenergic receptor

 

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.

Higenamine hydrochloride 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.
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
Molecular Weight

307.77

Formula

C16H18ClNO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC1=CC2=C(C(CC3=CC=C(O)C=C3)NCC2)C=C1O.[H]Cl
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
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)

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2492 mL 16.2459 mL 32.4918 mL
5 mM 0.6498 mL 3.2492 mL 6.4984 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, 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.

  • Molarity Calculator

  • 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: ≥ 2.08 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.
  • 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.

    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.

  • 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

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, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)

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: 99.68%

COA (251 KB) HNMR (266 KB) LCMS (83 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, 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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Higenamine hydrochloride 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:

Higenamine11041-94-4NorcoclaurineMDM-2/p53ROS KinaseApoptosisOsteoporosisLeukemiaMV4-11MOLM-13StrokeCRSC6HNPCsBMSCsInhibitorinhibitorinhibit

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