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Harmine PPAR modulator

Name: Harmine
Brand: Selleck Chemicals
SKU: S3868
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S3868

Harmine (Telepathine), a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. This compound also inhibits monoamine oxidases (MAOs), PPARγ and cdc-like kinases (CLKs). It inhibits 5-HT2A serotonin receptor with Ki of 397 nM.

Chemical Structure

Molecular Weight: 212.25

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Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Other PPAR Inhibitors	T0070907 GW9662 GW6471 WY-14643 (Pirinixic Acid) GSK3787 GW0742 AZ6102 GSK0660 Astaxanthin Eupatilin

Solubility

In vitro
Batch:

DMSO : 42 mg/mL (197.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.100mg/ml (9.89mM)	Taking the 1 mL working solution as an example, add 50 μL of 42 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.050mg/ml (4.95mM)	Taking the 1 mL working solution as an example, add 50 μL of 21 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	212.25	Formula	C₁₃H₁₂N₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	442-51-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Telepathine			Smiles	CC1=NC=CC2=C1NC3=C2C=CC(=C3)OC

Mechanism of Action

Targets/IC₅₀/Ki	PPARγ MAO-A (Cell-free assay) 0.048 μM(Ki)
In vitro	Harmine does not cause significant weight gain or hepatic lipid accumulation. It induces expression of both PPARγ1 and PPARγ2 in primary mouse bone-marrow-derived macrophages. This compound might promote the anti-inflammatory action of PPARγ in this cell type. It has previously been reported to interact with several cell-surface receptors, including monoamine oxidase A (MAO-A), serotonin receptor 2A (5-HT2A), imidazoline receptors (I1 and I2 sites), and cyclin-dependent kinases. This chemical has also been reported as a potent inhibitor of the dual specificity tyrosine-phosphorylation-regulated kinase (DYRK1A), which regulates cell proliferation and brain development. In fact, it also inhibits DYRK1B and DYRK2, but the efficiency of this inhibition is, respectively, 5- and 50-fold lower in comparison to DYRK1A. It can increase proliferation of human neural progenitors.
In vivo	Administration of harmine to diabetic mice mimics the effects of PPARγ ligands on adipocyte gene expression and insulin sensitivity. This compound does not cause significant weight gain or hepatic lipid accumulation. It regulates metabolic and inflammatory gene expression in vivo. Harmaline exhibits a dose-dependent bioavailability.
References	[1] https://pubmed.ncbi.nlm.nih.gov/17488638/ [2] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3629804/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06252506	Recruiting	Neuropharmacological Investigation of Ayahuasca Constituents DMT and Harmine	Insel Gruppe AG University Hospital Bern\|Psychiatric University Hospital Zurich	January 22 2024	Phase 1

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