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Lofepramine

Name: Lofepramine
Brand: TargetMol
SKU: T15773
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T15773Cas No. 23047-25-8

Alias Lopramine, Leo 640, Gamanil, Amplit

Lofepramine (Leo 640) is a potent tricyclic antidepressant that is extensively metabolized to desipramine. It inhibits the serotonin and norepinephrine transporters by inhibiting neurons with Kd values of 70 and 5.4 nM, respectively, with weak antagonism of serotonin, histamine and muscarinic receptors.

Lofepramine

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Purity: 98.38%

Catalog No. T15773Alias Lopramine, Leo 640, Gamanil, AmplitCas No. 23047-25-8

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$30	-	In Stock
2 mg	$40	-	In Stock
5 mg	$64	-	In Stock
10 mg	$89	-	In Stock
25 mg	$179	-	In Stock
50 mg	$272	-	In Stock
100 mg	$396	-	In Stock
200 mg	$589	-	In Stock
1 mL x 10 mM (in DMSO)	$71	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:98.38%

Appearance:Solid

Color:Yellow

Resource Download

COA HNMR HPLC

Product Introduction

Lofepramine AI Summary

Lofepramine exhibits diverse bioactivity profiles and some degree of pharmacokinetic complexity. It has a high partition coefficient (LogD = 4.58) and a slightly acidic pKa of 6.7, indicating possible pH-dependent solubility changes with a delta logD of -0.32 from pH 6.5 to 7.4. Despite these characteristics, its oral bioavailability in humans is low, with F ≤ 20.0%. This compound functions as an inhibitor across multiple biological targets. It inhibits acid sphingomyelinase (ASM) in human H4 cells (90.5% residual activity at 10 μM), Tyrosyl-DNA Phosphodiesterase (TDP1) with a potency of 44668.4 nM, and Bacillus subtilis Sfp phosphopantetheinyl transferase (PPTase) with potencies ranging from 15848.9 nM to 50118.7 nM. It also inhibits Histone Lysine Methyltransferase G9a (1258.9 nM), the vitamin D receptor (VDR) (35481.3-39810.7 nM), delayed death in malarial parasite plastid (12589.3-15101.4 nM), USP1/UAF1 (35481.3 nM), and induces DNA re-replication in various cell lines (33498.3 nM). However, it shows weak inhibitory activity in kinase assays against GST-RET proteins (IC50 > 20000.0 nM), and low potency in blocking uptake of substrates in human BSEP, MRP2, MRP3, and MRP4 transport proteins (IC50 > 133000.0 nM). In terms of antimicrobial activity, Lofepramine does not show significant effectiveness against Candida albicans, Cryptococcus neoformans, and various bacteria including Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Acinetobacter baumannii, and Staphylococcus aureus MRSA (MIC > 10000.0 nM). It also exhibits a high CC50 value for cytotoxicity against HEK293 cells (CC50 > 10000.0 nM). Despite moderate activity in certain viability assays against SARS-CoV-2-infected Vero E6 cells (inhibition index = 0.7416), it shows antiviral activity manifested by a 17.72% inhibition of SARS-CoV-2 cytotoxicity in Caco-2 cells at 10 μM after 48 hours and 64.61% inhibition of SARS-CoV-2 3CL-Pro protease at 20 μM. The IC50 value for VERO-6 cell cytotoxicity inhibition is greater than 20000.0 nM, indicating moderate to low potency. Lofepramine's activity includes 35.11% inhibition of human HDAC6 with a commercial substrate and 0.27% with a custom substrate, alongside various binding affinities and activities towards SLC6A2, SLC6A4, HRH1, DRD2, OPRK1, CHRM2, CNR1, NR1I2, HRH2, Ptgs1, and PDE4D. Liver toxicity has been associated with Lofepramine, including moderate hepatotoxicity (46.5% of cases), and acute liver toxicity characterized by cytolytic and choleostatic effects, though severe chronic liver diseases and secondary liver conditions are not significantly linked. Overall, Lofepramine shows potential as a multi-target inhibitor, with notable activity in certain pathways and processes, yet limited oral bioavailability and specific safety concerns necessitate cautious therapeutic consideration..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Lofepramine (Leo 640) is a potent tricyclic antidepressant that is extensively metabolized to desipramine. It inhibits the serotonin and norepinephrine transporters by inhibiting neurons with Kd values of 70 and 5.4 nM, respectively, with weak antagonism of serotonin, histamine and muscarinic receptors.
Targets&IC50	5-HT:70 nM(Kd), NET:5.4 nM(Kd)
Synonyms	Lopramine, Leo 640, Gamanil, Amplit

Chemical Properties

Molecular Weight	418.96
Formula	C₂₆H₂₇ClN₂O
Cas No.	23047-25-8
Smiles	C(CCN(CC(=O)C1=CC=C(Cl)C=C1)C)N2C=3C(CCC=4C2=CC=CC4)=CC=CC3
Relative Density.	1.173g/cm3

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 48 mg/mL (114.57 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 2 mg/mL (4.77 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3869 mL	11.9343 mL	23.8686 mL	119.3431 mL
5 mM	0.4774 mL	2.3869 mL	4.7737 mL	23.8686 mL
10 mM	0.2387 mL	1.1934 mL	2.3869 mL	11.9343 mL
20 mM	0.1193 mL	0.5967 mL	1.1934 mL	5.9672 mL
50 mM	0.0477 mL	0.2387 mL	0.4774 mL	2.3869 mL
100 mM	0.0239 mL	0.1193 mL	0.2387 mL	1.1934 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc