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LXE408 fumarate

Catalog No. T39214L
Synonyms: 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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
LXE408 fumarate Chemical Structure
LXE408 fumarate, CAS N/A
Pack Size Availability Price/USD Quantity
1 mg In stock $ 332.00
2 mg In stock $ 497.00
5 mg In stock $ 626.00
10 mg In stock $ 996.00
25 mg In stock $ 1,470.00
50 mg In stock $ 1,990.00
100 mg In stock $ 2,680.00
1 mL * 10 mM (in DMSO) In stock $ 923.00
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Purity: 98.10%
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Biological Description
Chemical Properties
Storage & Solubility Information
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)
Molecular Weight 559.51
Formula C27H22FN7O6

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5.6 mg/mL (10 mM)

TargetMolReferences and Literature

1. Advait Nagle, et al. Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of Leishmaniases. J Med Chem. 2020 Jul 15.

Related compound libraries

This product is contained In the following compound libraries:
Ubiquitination Compound Library

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Keywords

LXE408 fumarate Proteases/Proteasome Ubiquitination Proteasome LXE408 fumarate (1799330-15-6 Free base) LXE408 Fumarate 1799330-15-6 Free base LXE 408 Fumarate 1799330-15-6 LXE-408 Fumarate inhibitor inhibit

 

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