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-Phe-Arg-pNA
Z-Phe-Arg-pNA is a substrate of Cathepsin L. |
| LN5P45
LN5P45 is an OTUB2 inhibitor (IC50: 2.3 μM). |
| TSC25
TSC25 is a potent cruzipain (CZP) inhibitor, with an IC50 of 3.34 nM and a pIC50 of 8.48. |
| Ac-VLPE-FMK
Ac-VLPE-FMK, a tetrapeptidyl mono-fluoromethyl ketone (m-FMK), is a Cat-B and Cat-L inhibitor. |
| p-Aminophenylmercuric acetate
p-Aminophenylmercuric acetate is an organomercurial activator of matrix metalloproteinases (MMP). |
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