GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC50=0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC50: purified 26S=13 µM; enriched THP-1 extracts IC50=40µM). GSK3494245 exhibits attractive biological and biosafety properties.
| Molecular Weight | 410.44 |
| Formula | C21H23FN6O2 |
| CAS Number | 2080410-41-7 |
| Form | Solid |
| Solubility (25°C) | DMSO 100 mg/mL (ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
| Related Parasite Products |
|---|
| Argifin
Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms. |
| Argadin
Argadin is a cyclopentapeptide chitinase inhibitor. |
| DABCYL-Glu-Arg-Nle-Phe-Leu-Ser-Phe-Pro-EDANS
DABCYL-Glu-Arg-Nle-Phe-Leu-Ser-Phe-Pro-EDANS is a fluorescent dye, and can be applied in a fluorogenic substrate for an aspartyl proteinase from human malaria parasite. |
| Xenopsin precursor fragment
Xenopsin precursor fragment is an antimicrobial peptide, and has antibacterial/antifungal (10-500 μg/mL) and anti-protozoal (MIC: 2-20 μg/mL) activity. |
| Dihydrocyclosporin A
Dihydrocyclosporin A is a derivative of Cyclosporine A. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
