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2 or test compound) and 80 μL of purified granulocytes. After incubation at 37 °C for 15 min, the cells were fixed and incubated in the dark for a further 15 min at room temperature. Remaining red blood cells were lysed using a hypotonic shock. The level of CD11b expression was determined by flow cytometry using lack of CD16 expression to distinguish eosinophils from neutrophils.
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42149195403
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At other biological targets, partial agonists or antagonists have had consistently higher lipophilicity than would be expected for an agonist of comparable affinity. See for example
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At other biological targets, partial agonists or antagonists have had consistently higher lipophilicity than would be expected for an agonist of comparable affinity. See for example: Parker, M. A.; Kurrasch, D. M.; Nichols, D. E. Bioorg. Med. Chem. 2008, 16, 4661.
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71049187691
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Dilute bovine serum albumin was used as part of the buffer medium for cost reasons. This is relatively commonplace see for example At these dilute serum albumin concentrations and with relatively free compounds this approximation is expected to have minimal impact. However, significant differences between protein shifts across species can occur, and so independent plasma protein binding measurements in 100% plasma were undertaken for 34 across multiple species. Relatively consistent values were obtained: human 4.6, rat 5.6, dog 3.0, cyno 2.6 (% free)
-
Dilute bovine serum albumin was used as part of the buffer medium for cost reasons. This is relatively commonplace (see for example Liu, J.; Fu, Z.; Wang, Y.; Schmitt, M.; Huang, A.; Marshall, D.; Tonn, G.; Seitz, L.; Sullivan, T.; Tang, H. L.; Collins, T.; Medina, J. Bioorg. Med. Chem. Lett. 2009, 19, 6419. ). At these dilute serum albumin concentrations and with relatively free compounds this approximation is expected to have minimal impact. However, significant differences between protein shifts across species can occur, and so independent plasma protein binding measurements in 100% plasma were undertaken for 34 across multiple species. Relatively consistent values were obtained: human 4.6, rat 5.6, dog 3.0, cyno 2.6 (% free)..
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22
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79957858840
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note
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3N requires C, 52.7; H, 4.5; N, 1.5; S, 7.8%. Found: C, 52.4; H, 4.5; N, 1.2; S, 7.8%.
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23
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84864171299
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online. See
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Sargent, C.; Stinson, S.; Schmidt, J.; Dougall, I.; Bonnert, R.; Paine, S.; Saunders, M.; Foster, M. Br. J. Pharmacol. 2009, 98, pA2 online. (See https://bps.conference-services.net/resources/344/1686/pdf/JB2009-0098.pdf).
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