Brief introduction of 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Application In Synthesis of 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 1750-45-4, name is 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one. In an article£¬Which mentioned a new discovery about 1750-45-4

The tyrosine kinase inhibitor nilotinib selectively inhibits cyp2c8 activities in human liver microsomes

The tyrosine kinase inhibitor nilotinib was examined for its inhibition of cytochrome P450s (CYPs) in human liver microsomes and in human CYPs expressed in a baculovirus-insect cell system. Nilotinib demonstrated preferential inhibition of CYP2C8-mediated paclitaxel 6alpha-hydroxylation, rosiglitazone hydroxylation and amodiaquine N-deethylation in human liver microsomes, with IC50 values of 0.4, 7.5 and 0.7 muM, respectively. The IC 50 value of nilotinib for paclitaxel 6alpha-hydroxylation was 20-fold lower than that of the other five tyrosine-kinase inhibitors tested. Nilotinib appears to display competitive inhibition against paclitaxel 6alpha-hydroxylation and amodiaquine N-deethylation, with estimated mean Ki values of 0.90 and 0.15 muM in human liver microsomes and 0.10 and 0.61 muM in recombinant human CYP2C8, respectively. These results are consistent with those of molecular docking simulations, where paclitaxel could not access the CYP2C8 catalytic site in the presence of nilotinib, but the binding of midazolam, a substrate of CYP3A4, to the catalytic site of CYP3A4 was not affected by nilotinib. The demonstrated inhibitory activity of nilotinib against CYP2C8 at concentrations less than those observed in patients who received nilotinib therapy is of potential clinical relevance and further in vivo exploration is warranted.

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Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem