Free shipping on all orders over $ 500

LXE408

Cat. No. M21267
LXE408  Structure
Size Price Availability
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

LXE408 is an oral antileishmanarial compound that selectively targets the kinetoplastid proteosome vs. the mammalian proteosome.

Chemical Information
Molecular Weight 443.43
Formula C23H18FN7O2
CAS Number 1799330-15-6
Solubility (25°C) DMSO : 16.67 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Mohd Imran, et al. Expert Opin Ther Pat. Small molecules as kinetoplastid specific proteasome inhibitors for leishmaniasis: a patent review from 1998 to 2021

[2] Advait Nagle, et al. J Med Chem. Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of Leishmaniases

Related Proteasome Products
NIC-0102

NIC-0102 is an orally potent proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammasome activation.NIC-0102 showed potent anti-inflammatory effects in vivo in a DSS-induced ulcerative colitis model. In addition, NIC-0102 inhibited the production of pro-IL-1β.

Ac-WLA-AMC

Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate.

Ac-Nle-Pro-Nle-Asp-AMC

Ac-Nle-Pro-Nle-Asp-AMC is a specific substrate for 26S proteasome.

PR-39

PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor.

PSI

PSI (Proteasome Inhibitor 1) is a potent proteasome inhibitor.

  Catalog
Abmole Inhibitor Catalog




Keywords: LXE408 supplier, Proteasome, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.