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Imipramine HCl Serotonin Transporter inhibitor

Name: Imipramine HCl
Brand: Selleck Chemicals
SKU: S4377
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S4377

Imipramine (Melipramine,G 22355) is a tricyclic antidepressant (TCA) of the dibenzazepine group, mainly used in the treatment of major depression and enuresis (inability to control urination).

Chemical Structure

Molecular Weight: 316.87

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Quality Control

Batch: Purity: 99.95%

99.95

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE)
Other Serotonin Transporter Inhibitors	Dapoxetine

Solubility

In vitro
Batch:

DMSO : 63 mg/mL (198.81 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 63 mg/mL

Ethanol : 63 mg/mL

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.
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.	3.150mg/ml (9.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 63 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.	0.780mg/ml (2.46mM)	Taking the 1 mL working solution as an example, add 50 μL of 15.6 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

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.

Chemical Information, Storage & Stability

Molecular Weight	316.87	Formula	C₁₉H₂₅ClN₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	113-52-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Melipramine HCl,G 22355			Smiles	CN(C)CCCN1C2=CC=CC=C2CCC3=CC=CC=C31.Cl

Mechanism of Action

In vitro	Imipramine in the microsomal incubation results in a predicted value for human clearance of 8.6 to 11 ml/min/kg, a slight underestimate of reported mean human blood clearance values (14–15 ml/min/kg). Imipramine is metabolized into N-desmethylimipramine (84%), 2-hydroxyimipramine (10%), and 10-hydroxyimipramine (6%) in human hepatic microsomes. Imipramine (3 μM) inhibits HERG-encoded potassium channels in a reversible manner in CHO cells. Imipramine (3 μM) inhibits HERG tail currents (IHERG) following test pulses to +20 mV with an IC50 of 3.4 μM and a Hill coefficient of 1.17 in CHO cells. Imipramine can completely block native cardiac IKr at 1μm in guinea-pig myocytes.
In vivo	Imipramine (10 mg/kg b.i.d.) reverses the decreased sucrose intake of rats exposed to chronic mild stress. Imipramine (10 mg/kg b.i.d.) completely reverses stress caused decrease in D2-receptor binding in the limbic forebrain (but not the striatum). Imipramine (15 mg/kg, IP) exerts anxiolytic-like effects in the two elevated T-maze tasks in male Wistar rats. Imipramine (15 mg/kg, IP) enhances both avoidance and escape latencies in male Wistar rats. Imipramine (15 mg/kg, IP) decreases locomotor activity measured in a square arena in male Wistar rats.
References	[1] https://pubmed.ncbi.nlm.nih.gov/9394025/ [2] https://pubmed.ncbi.nlm.nih.gov/8502233/ [3] https://pubmed.ncbi.nlm.nih.gov/10510461/ [4] https://pubmed.ncbi.nlm.nih.gov/7871087/ [5] https://pubmed.ncbi.nlm.nih.gov/10764908/

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06312813	Recruiting	Rosacea	Wright State University	February 27 2024	Phase 2
NCT04520217	Recruiting	Photosensitivity\|Microvesicle Particle	Wright State University	June 6 2022	Phase 1
NCT00693680	Completed	Major Depression	Polish Academy of Sciences\|Jagiellonian University	January 2005	Not Applicable

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