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Fig. 1 | Skeletal Muscle

Fig. 1

From: Pharmacology and macrophage modulation of HPGDS inhibitor PK007 demonstrate reduced disease severity in DMD-affected muscles of the mdx mouse model

Fig. 1

In vitro studies demonstrated nanomolar potency and showed excellent pharmacokinetics of PK007. A displays the inhibitory activity of PK007 on PGD2 concentration (%) via fluorescence polarisation (FP) enzyme-based assays, where potency was 1.54 ± 0.26 µM. The assay was conducted with triplicate replicates, with over three assays (n = 3). B The cell-based potency of PK007, when measured via PGD2-MOX ELISA in LPS-stimulated macrophages, showed that the inhibition of PGD2 was 17.23 ± 12 nM. The assay was conducted in technical duplicates or triplicates over four assays (n = 4). GraphPad Prism software utilised a non-linear regression algorithm for log (concentration) versus normalised response. C Pharmacokinetics to determine the in vivo half-life of PK007 in blood plasma was determined in C57BL/6 mice, using two different delivery regimens (n = 3 for each treatment), orally (PO, 10 mg/kg) and intravenously (IV, 2 mg/kg). The sampling time was over 24 h (hrs), and plasma concentration was measured (nM). Pharmacokinetic evaluations were conducted by WuXi AppTec (Shanghai, China). Data are shown as mean ± SEM

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Skeletal Muscle

ISSN: 2044-5040

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