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  3. 9-Methyl-β-carboline

9-Methyl-β-carboline is a monoamine oxidase inhibitor and dopaminergic modulator, with an IC50 of 1 μM against human MAO-A and an IC50 of 15.5 μM against human MAO-B. 9-Methyl-β-carboline possesses cognitive enhancement potential and can cross the blood-brain barrier. 9-Methyl-β-carboline increases dopamine levels by inhibiting monoamine oxidase activity and microglial proliferation. 9-Methyl-β-carboline activates PKA/PKC and mitochondrial respiratory chain complex I, promotes neurotrophic factor expression and reduces α-synuclein (α-synuclein) levels, thereby reversing neurotoxin-induced dopaminergic neuron damage. 9-Methyl-β-carboline also regulates the PI3K pathway and exerts an anti-proliferative effect on astrocytes. 9-Methyl-β-carboline is widely used in Parkinson's disease-related studies.

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9-Methyl-β-carboline

9-Methyl-β-carboline Chemical Structure

CAS No. : 2521-07-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
500 mg In-stock
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5 g   Get quote  

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

9-Methyl-β-carboline is a monoamine oxidase inhibitor and dopaminergic modulator, with an IC50 of 1 μM against human MAO-A and an IC50 of 15.5 μM against human MAO-B. 9-Methyl-β-carboline possesses cognitive enhancement potential and can cross the blood-brain barrier. 9-Methyl-β-carboline increases dopamine levels by inhibiting monoamine oxidase activity and microglial proliferation. 9-Methyl-β-carboline activates PKA/PKC and mitochondrial respiratory chain complex I, promotes neurotrophic factor expression and reduces α-synuclein (α-synuclein) levels, thereby reversing neurotoxin-induced dopaminergic neuron damage. 9-Methyl-β-carboline also regulates the PI3K pathway and exerts an anti-proliferative effect on astrocytes. 9-Methyl-β-carboline is widely used in Parkinson's disease-related studies[1][2][3][4].

IC50 & Target

hMAO-A

1 μM (IC50)

hMAO-B

15.5 μM (IC50)

In Vitro

9-Methyl-β-carboline increases the number of dopaminergic neurons and promotes neurite branching in primary midbrain cultures[1].
9-Methyl-β-carboline (90 μM; 48 h) is taken up by primary dopaminergic neurons via DAT, and increases the number of THir neurons by 30% (peak at 90 μM for 48 h) by upregulating TH expression in pre-existing non-proliferative DDCir neurons; this effect is partially reversible after drug withdrawal and depends on the PKA/C signaling pathway[2].
9-Methyl-β-carboline (10-150 μM; 48 h) exerts a concentration-dependent antiproliferative effect on primary mouse cortical astrocytes[4].
9-Methyl-β-carboline (90 μM; 48 h) significantly upregulates the expression of multiple neurotrophic factors and related genes in primary mouse cortical astrocyte cultures[4].
The stimulatory effect of 9-Methyl-β-carboline (90 μM; 48 h) on the number of tyrosine hydroxylase-immunoreactive dopaminergic neurons in primary mouse midbrain cell cultures is mediated by the phosphatidylinositol 3-kinase (PI3K) pathway[4].

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

Cell Proliferation Assay[4]

Cell Line: Primary murine cortical astrocytes
Concentration: 10 μM, 30 μM and 50 μM
Incubation Time: 48 h
Result: Exerted anti-proliferative effects on primary murine cortical astrocytes in a concentration-dependent manner, reducing BrdU incorporation by 39 ± 4% at 90 μM and 71 ± 6% at 150 μM for 48 h.
In Vivo

9-Methyl-β-carboline (2 μmol/100 g body weight; i.p.; daily; 10 days) improves hippocampus-dependent spatial learning in female Wistar rats, associated with a significant increase in hippocampal dopamine levels and enhanced dendritic and synaptic proliferation in dentate gyrus granule neurons, while 9-Methyl-β-carboline (2 μmol/100 g body weight; i.p.; daily; 5 days) shows no significant PD effects[1].
9-Methyl-β-carboline (0.48 μmol/kg) restores the number of THir neurons in the SN pars compacta of MPP+-treated rats, upregulates neurotrophic factor expression, and enhances mitochondrial complex I activity[2].
9-Methyl-β-carboline (0.105 mg/kg/day; intracerebroventricular; continuous infusion; 14 days) exerts restorative effects in a rat model of Parkinson’s disease, normalizing striatal dopamine levels and THir cell counts in the SNc, increasing mitochondrial complex I activity by ~80%, and strongly upregulating neurotrophin gene and protein expression[3].
9-Methyl-β-carboline exerts neuroregenerative effects in an MPP+-induced rat model of Parkinson's disease and increases expression of key neurotrophic factors[4].

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

Animal Model: Wistar (female, 7 weeks old at study start)[1]
Dosage: 2 μmol/100 g body weight (10-day treatment: spatial learning, dopamine levels, dendritic/synaptic changes); 2 μmol/100 g body weight (5-day treatment: no significant effects)
Administration: i.p.; daily; 5 days followed by 5 days vehicle; daily; 10 days
Result: Reduced spatial learning errors in radial maze, with rats reaching ≤1 error criterion after 7 training trials; confirmed significant treatment effect on test acquisition with significant differences vs.
controls from trial 7 onward (10-day treatment only).
Significantly increased hippocampal dopamine levels to ~14 ng/g wet weight, with significant elevations vs.
non-injected and vehicle-treated rats (10-day treatment only).
Significantly increased dendritic length of dentate gyrus granule neurons at 60 μm, 110 μm, and 160 μm from the soma (10-day treatment only).
Significantly increased total dendritic spine number per tree at 60 μm, 110 μm, and 160 μm from the soma (10-day treatment only).
Significantly increased dendritic complexity (number of dendritic intersections) at 110 μm from the soma (10-day treatment only).
Showed no significant difference from controls in spatial learning, no significant hippocampal dopamine elevation, and no significant dendritic/synaptic changes (5-day treatment only).
Molecular Weight

182.22

Formula

C12H10N2

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CN1C2=C(C=CC=C2)C3=C1C=NC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Store at room temperature 3 years

In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (548.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.4879 mL 27.4394 mL 54.8787 mL
5 mM 1.0976 mL 5.4879 mL 10.9757 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (27.44 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (27.44 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
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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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).
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
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 5.4879 mL 27.4394 mL 54.8787 mL 137.1968 mL
5 mM 1.0976 mL 5.4879 mL 10.9757 mL 27.4394 mL
10 mM 0.5488 mL 2.7439 mL 5.4879 mL 13.7197 mL
15 mM 0.3659 mL 1.8293 mL 3.6586 mL 9.1465 mL
20 mM 0.2744 mL 1.3720 mL 2.7439 mL 6.8598 mL
25 mM 0.2195 mL 1.0976 mL 2.1951 mL 5.4879 mL
30 mM 0.1829 mL 0.9146 mL 1.8293 mL 4.5732 mL
40 mM 0.1372 mL 0.6860 mL 1.3720 mL 3.4299 mL
50 mM 0.1098 mL 0.5488 mL 1.0976 mL 2.7439 mL
60 mM 0.0915 mL 0.4573 mL 0.9146 mL 2.2866 mL
80 mM 0.0686 mL 0.3430 mL 0.6860 mL 1.7150 mL
100 mM 0.0549 mL 0.2744 mL 0.5488 mL 1.3720 mL
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9-Methyl-β-carboline
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