1. Metabolic Enzyme/Protease
    Anti-infection
  2. Proteasome
    Parasite
  3. LXE408

LXE408 

Cat. No.: HY-131350
Handling Instructions

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

For research use only. We do not sell to patients.

LXE408 Chemical Structure

LXE408 Chemical Structure

CAS No. : 1799330-15-6

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

LXE408 is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. LXE408 has a low propensity to cross the blood brain barrier. LXE408 has the potential for visceral leishmaniasis (VL) research[1].

In Vitro

LXE408 (compound 1) can occupy the pocket as a ternary complex with the proteasome. LXE408 shows no inhibition of the hERG channel (IC50>30 μM) in a manual patch clamp assay. LXE408 has a low propensity to cross the blood brain barrier (brain/plasma AUC ratio=0.03 in mice)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

LXE408 (compound 1; 0.3-10 mg/kg; PO; twice daily for 8 days) potently reduces the parasite burden in the liver in a dose-dependent manner[1].
LXE408 (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[1].
LXE408 (5 mg/kg IV and 20 mg/kg PO) has a T1/2 of 3.3 hours for mouse. LXE408 (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[1].
LXE408 (0.3 mg/kg IV and 1.0 mg/kg PO) has a T1/2 of 3.8 hours for male beagle dog. LXE408 (0.3 mg/kg IV and 10 mg/kg PO) has a T1/2 of 9.7 hours for male cynomolgus monkey[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c mice (6-8 weeks old) infected with L. donovani[1]
Dosage: 0.3, 1, 3, 10 mg/kg
Administration: PO; twice daily for 8 days
Result: Led to a 95% and >99.84% reduction of parasite burden in the liver at 1 mg/kg and 10 mg/kg.
Animal Model: Balb/C mice[1]
Dosage: 5 mg/kg IV and 20 mg/kg PO (Pharmacokinetic Analysis)
Administration: IV or PO
Result: Had a T1/2 of 3.3 hours, a CL of 2.3 mL/min•kg, and a Vss of 0.63 L/kg for mouse.
Molecular Weight

443.43

Formula

C₂₃H₁₈FN₇O₂

CAS No.

1799330-15-6

SMILES

O=C(C1=C(C)N=C(C)O1)NC2=CC=C(F)C(C3=NN4C=C(C5=NC=CC=C5C)C=NC4=N3)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

LXE408LXE 408LXE-408ProteasomeParasitekinetoplastidL.donovaniVisceralleishmaniasishERGInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
LXE408
Cat. No.:
HY-131350
Quantity:
MCE Japan Authorized Agent: