≥99% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.
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Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
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Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Overview
LXE408 is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 has an IC 50 of 0.04 μM for L. donovani proteasome and an EC 50 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.
In Vitro
LXE408 (compound 1) can occupy the pocket as a ternary complex with the proteasome. LXE408 shows no inhibition of the hERG channel (IC 50 >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). 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 . 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 . LXE408 (5 mg/kg IV and 20 mg/kg PO) has a T 1/2 of 3.3 hours for mouse. LXE408 (3 mg/kg IV and 10 mg/kg PO) has a T 1/2 of 3.8 hours, a CL of 2.1 mL/min•kg, and a V ss of 0.53 L/kg for male Sprague-Dawley rat . LXE408 (0.3 mg/kg IV and 1.0 mg/kg PO) has a T 1/2 of 3.8 hours for male beagle dog. LXE408 (0.3 mg/kg IV and 10 mg/kg PO) has a T 1/2 of 9.7 hours for male cynomolgus monkey . 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 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 Dosage: 5 mg/kg IV and 20 mg/kg PO (Pharmacokinetic Analysis) Administration: IV or PO Result: Had a T 1/2 of 3.3 hours, a CL of 2.3 mL/min•kg, and a V ss of 0.63 L/kg for mouse.
LXE408 is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 has an IC 50 of 0.04 μM for L. donovani proteasome and an EC 50 of 0.04 μM for L. donovani . LXE408 has a low propensity to cross the blood brain barrier.
Storage
Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
This compound belongs to the class of organic compounds known as aromatic anilides. These are aromatic compounds containing an anilide group in which the carboxamide group is substituted with an aromatic group. They have the general structure RNC(=O)R', where R= benzene, and R = aryl group.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
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