SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 quarterhydrate inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 quarterhydrate shows no inhibitory activity against cathepsin G.
| Molecular Weight | 544.16 |
| Solubility (25°C) | DMSO 50 mg/mL Ethanol 5 mg/mL |
| 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 Cathepsin Products |
|---|
| Z-Gly-Pro-Arg-AMC hydrochloride
Z-Gly-Pro-Arg-AMC hydrochloride a fluorescent trypsin and cathepsin K substrate. |
| N-CBZ-Phe-Arg-AMC
N-CBZ-Phe-Arg-AMC (Z-FR-AMC) is a cathepsin substrate used in assessment activity of lysosomal cathepsin enzymes. |
| Ac-Glu-Asp(EDANS)-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Gly-Lys(DABCYL)-Glu-NH2
Ac-Glu-Asp(EDANS)-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Gly-Lys(DABCYL)-Glu-NH2 is a cathepsin D substrate, that can be used for cathepsin D FRET assay. |
| (S, S)-Z-FA-FMK
(S,S)-Z-FA-FMK is a cell-permeable, irreversible cathepsin B inhibitor. |
| H-Pro-Thr-Glu-Phe-p-nitro-Phe-Arg-Leu-OH
H-Pro-Thr-Glu-Phe-p-nitro-Phe-Arg-Leu-OH is a water-soluble polypeptide that can serve as a substrate for cathepsin D, pepsin and pepsinogen. |
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