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LXE408 fumarate

Name: LXE408 fumarate
Brand: TargetMol
SKU: T39214L
Price: 332 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T39214L

Alias LXE408 fumarate (1799330-15-6 Free base)

LXE408 fumarate is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 fumarate has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. LXE408 fumarate has a low propensity to cross the blood brain barrier. LXE408 fumarate has the potential for visceral leishmaniasis (VL) research.

LXE408 fumarate

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Purity: 99.89%

Catalog No. T39214LAlias LXE408 fumarate (1799330-15-6 Free base)

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$332	-	In Stock
2 mg	$497	-	In Stock
5 mg	$626	-	In Stock
10 mg	$996	-	In Stock
25 mg	$1,470	-	In Stock
50 mg	$1,990	-	In Stock
100 mg	$2,680	-	In Stock
1 mL x 10 mM (in DMSO)	$923	-	In Stock

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

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Purity:99.89%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	LXE408 fumarate is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 fumarate has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. LXE408 fumarate has a low propensity to cross the blood brain barrier. LXE408 fumarate has the potential for visceral leishmaniasis (VL) research.
In vitro	LXE408 fumarate occupy the pocket as a ternary complex with the proteasome. In a manual patch clamp assay, LXE408 fumarate shows no inhibition of the hERG channel (IC50>30 μM). LXE408 fumarate has a low propensity to cross the blood brain barrier (brain/plasma AUC ratio=0.03 in mice)[1].
In vivo	LXE408 fumarate ( 0.3-10 mg/kg; PO; twice daily for 8 days) potently reduces the parasite burden in the liver in a dose-dependent manner. LXE408 fumarate (1, 3, 10, 20 mg/kg; p.o.; b.i.d.; for 10 days) effects robust healing of parasite-induced skin lesions at the base of the tail in BALB/c mice infected with L. major. LXE408 fumarate (5 mg/kg IV and 20 mg/kg PO) has a T1/2 of 3.3 hours for mouse. LXE408 fumarate (3 mg/kg IV and 10 mg/kg PO) has a T1/2 of 3.8 hours, a CL of 2.1 mL/min•kg, and a Vss of 0.53 L/kg for male Sprague-Dawley rat. LXE408 fumarate (0.3 mg/kg IV and 1.0 mg/kg PO) has a T1/2 of 3.8 hours for male beagle dog. LXE408 fumarate (0.3 mg/kg IV and 10 mg/kg PO) has a T1/2 of 9.7 hours for male cynomolgus monkey[1].
Synonyms	LXE408 fumarate (1799330-15-6 Free base)

Chemical Properties

Molecular Weight	559.51
Formula	C₂₇H₂₂FN₇O₆
Smiles	OC(=O)\C=C\C(O)=O.Cc1nc(C)c(o1)C(=O)Nc1ccc(F)c(c1)-c1nc2ncc(cn2n1)-c1ncccc1C
Relative Density.	no data available

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: 5.6 mg/mL (10.01 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7873 mL	8.9364 mL	17.8728 mL	89.3639 mL
5 mM	0.3575 mL	1.7873 mL	3.5746 mL	17.8728 mL
10 mM	0.1787 mL	0.8936 mL	1.7873 mL	8.9364 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