research use only
Cat.No.S4246
|
In vitro |
DMSO
: 34 mg/mL
(200.41 mM)
Water : 34 mg/mL Ethanol : 34 mg/mL |
|
In vivo |
|||||
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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.)
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.
| Molecular Weight | 169.65 | Formula | C9H12ClN |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 1986-47-6 | Download SDF | Storage of Stock Solutions |
|
|
| Synonyms | 2-PCPA HCl, SKF-385 HCl | Smiles | C1C(C1N)C2=CC=CC=C2.Cl | ||
| Targets/IC50/Ki |
MAO-B
(Cell-free assay) 7 μM
MAO-A
(Cell-free assay) 11.5 μM
LSD1
(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. Tranylcypromine (500 μg/mL) severely inhibits bradykinin-stimulated arachidonic acid release in calf aortic endothelial cells. 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.
|
| 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.
|
References |
|
(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 |
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.