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Inhibition of CYP2C19 in human liver microsomes at 25 uM in the presence of NADPH
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of CYP2C9 in human liver microsomes at 25 uM in the presence of NADPH
Cmax in Sprague-Dawley rat at 5 mg/kg, iv
SummaryCompounds, ActivePubMed Citation
Inhibition of PDE10A (449 to 770 residues) (unknown origin) expressed in Escherichia coli BL21 using [3H]-cAMP as substrate measured for 15 mins by liquid scintillation counter method
Inhibition of PDE7A1 (130-482 residues) (unknown origin) expressed in Escherichia coli BL21 using [3H]-cAMP as substrate measured for 15 mins by liquid scintillation counter method
Inhibition of PDE5A1 (535 to 860 residues) (unknown origin) expressed in Escherichia coli BL21 [3H]-cGMP as substrate measured for 15 mins by liquid scintillation counter method
Inhibition of PDE4B2 (152 to 487 residues) (unknown origin) expressed in Escherichia coli BL21 measured for 15 mins by liquid scintillation counter method
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of PDE2A (580 to 919 residues) (unknown origin) expressed in Escherichia coli BL21 using [3H]-cGMP as substrate measured for 15 mins by liquid scintillation counter method
Inhibition of PDE1B (10 to 487 residues) (unknown origin) expressed in Escherichia coli BL21 using [3H]-cGMP as substrate measured for 15 mins by liquid scintillation counter method
Inhibition of PDE1A (142 to 552 residues) (unknown origin) expressed in Escherichia coli BL21 measured for 15 mins by liquid scintillation counter method
Inhibition of PDE4D2 (86 to 413 residues) (unknown origin) expressed in Escherichia coli BL21 [3H]-cAMP as substrate measured for 15 mins by liquid scintillation counter method
Inhibition of PDE1C (147 to 531 residues) (unknown origin) expressed in Escherichia coli BL21 using [3H]-cGMP as substrate measured for 15 mins by liquid scintillation counter method
Assay data:13 Active, 8 Activity ≤ 1 µM, 14 Tested
Antifibrotic activity in bleomycin-induced Sprague-Dawley rat pulmonary fibrosis model assessed as smaller lung foci at 5 mg/kg, ip administered daily for 28 days by H&E staining based histopathological analysis
Antifibrotic activity in bleomycin-induced Sprague-Dawley rat pulmonary fibrosis model assessed as decrease in number of lung foci at 5 mg/kg, ip administered daily for 28 days by H&E staining based histopathological analysis
Antifibrotic activity in TGF-beta induced HLF cell assessed as decrease in alpha-SMA level at 10 to 20 uM incubated for 48 hrs by DAPI staining based immunofluorescence microscopic analysis
Antifibrotic activity in TGF-beta induced HLF cell assessed as decrease in FN level at 10 to 20 uM incubated for 48 hrs by DAPI staining based immunofluorescence microscopic analysis
Antifibrotic activity in TGF-beta induced HLF cell assessed as suppression of FN level at 10 uM incubated for 48 hrs by Western blot analysis
Antifibrotic activity in TGF-beta induced HLF cell assessed as suppression of alpha-SMA level at 10 uM incubated for 48 hrs by Western blot analysis
Antifibrotic activity in TGF-beta induced HLF cell assessed as suppression of Col-I level at 10 uM incubated for 48 hrs by Western blot analysis
Antifibrotic activity in bleomycin-induced Sprague-Dawley rat lung fibrosis model assessed as increase in cGMP level at 2.5 to 5 mg/kg, ip administered daily for 28 days by ELISA analysis
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