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Tranylcypromine HCl MAO inhibitor

Name: Tranylcypromine HCl
Brand: Selleck Chemicals
SKU: S4246
Availability: InStock
Rating: 5 (18 reviews)

Cat.No.S4246

Tranylcypromine HCl is a monoamine oxidase inhibitor, which inhibits CYP2A6 with K_i of 0.08 μM and 0.2 μM in cDNA-expressing microsomes and Human Liver Microsomes, respectively.

Chemical Structure

Molecular Weight: 169.65

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.91%

99.91

Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE phosphatase PPAR HSP (HSP90) Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase Serine/threonin kinase Lipoxygenase Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Fatty Acid Synthase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR IDO/TDO Hydroxylase PCSK9 OXPHOS ROR
Related Products	Moclobemide (Ro 111163) Sennoside A Paeonol J147 Isatin

Chemical Information, Storage & Stability

Molecular Weight	169.65	Formula	C₉H₁₂ClN	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1986-47-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	2-PCPA HCl, SKF-385 HCl			Smiles	C1C(C1N)C2=CC=CC=C2.Cl

Solubility

In vitro
Batch:

DMSO : 34 mg/mL ( (200.41 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 34 mg/mL

Ethanol : 34 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.
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.	1.700mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 34 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.	0.425mg/ml (2.51mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.5 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.
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.

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 Number of animals:

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+ %

Calculation results:

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.

Mechanism of Action

Targets/IC₅₀/Ki	MAO-B ^[5] (Cell-free assay) 7 μM MAO-A ^[1] (Cell-free assay) 11.5 μM LSD1 ^[5] (Cell-free assay) 22.3 μM
In vitro	R-(+)-Tranylcypromine, (±)-Tranylcypromine, and S-(−)-Tranylcypromine competitively inhibits CYP2A6-mediated metabolism of nicotine with apparent Ki values of 0.05 μM, 0.08 μM, and 2.0 μM, respectively, in human liver microsomes. ^[1] Tranylcypromine (500 μg/mL) severely inhibits bradykinin-stimulated arachidonic acid release in calf aortic endothelial cells. ^[2] Tranylcypromine inhibits CYP2A6 and CYP2E1 activity with IC50 of 0.42 μM and 3 μM, respectively, in human liver microsomes. Tranylcypromine induces type II and cyclopropylbenzene type I difference spectrum in human liver microsomes. ^[3]
In vivo	Tranylcypromine injection leads to a large, slow increase in motor activity at 5 mg/kg and 10 mg/kg compared with the saline control in male rats, although 2 mg/kg Tranylcypromine does not induce an increase. Tranylcypromine (10 mg/kg) also causes significant decreases in the number of rearing behaviors in male rats. ^[4]
References	https://pubmed.ncbi.nlm.nih.gov/11353760/ https://pubmed.ncbi.nlm.nih.gov/6776101/ https://pubmed.ncbi.nlm.nih.gov/11181487/ https://pubmed.ncbi.nlm.nih.gov/15289160/ https://pubmed.ncbi.nlm.nih.gov/29031059/

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04841798	Completed	Major Depressive Disorder\|Treatment Resistant Depression	Centre for Addiction and Mental Health	April 15 2021	Not Applicable

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