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Microcystin-LR is a potent protein phosphatase inhibitor with IC50 of 0.04 nM for PP2A, >40-fold selectivity over PP1.
Comp Biochem Physiol C Toxicol Pharmacol. 2018 Aug;210:18-29.
Structural and functional analysis of two novel somatostatin receptors identified from topmouth culter (Erythroculter ilishaeformis)
Microcystin-LR purchased from AbMole
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Source | Comp Biochem Physiol C Toxicol Pharmacol (2018). Figure 6. MC-LR (AbMole BioScience,Shanghai, China) |
| Method | qRT-PCR | |
| Cell Lines | fish | |
| Concentrations | 2 μg/L, 20 μg/L | |
| Incubation Time | 30 days | |
| Results | In the brain, the transcription of the two receptors was increased after MC-LR treatment, whereas in the liver and spleen, it was markedly upregulated at low MC-LR concentration (2 μg/L) and downregulated at high MC-LR concentration (20 μg/L) compared with the control group |
| Molecular Weight | 995.17 |
| Formula | C49H74N10O12 |
| CAS Number | 101043-37-2 |
| Solubility (25°C) | Ethanol ≥ 0.5 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.
[1] Yaqoob Lone, et al. J Toxicol. Microcystin-LR Induced Immunotoxicity in Mammals
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