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| | Methanone, [(4aR)-1-(4-fluorophenyl)-1,4,5,6,7,8-hexahydro-6-[[4-(trifluoromethyl)phenyl]sulfonyl]-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl]-2-pyridinyl- Basic information |
| Product Name: | Methanone, [(4aR)-1-(4-fluorophenyl)-1,4,5,6,7,8-hexahydro-6-[[4-(trifluoromethyl)phenyl]sulfonyl]-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl]-2-pyridinyl- | | Synonyms: | Methanone, [(4aR)-1-(4-fluorophenyl)-1,4,5,6,7,8-hexahydro-6-[[4-(trifluoromethyl)phenyl]sulfonyl]-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl]-2-pyridinyl-;CORT113176;Dazucorilant | | CAS: | 1496508-34-9 | | MF: | C29H22F4N4O3S | | MW: | 582.57 | | EINECS: | | | Product Categories: | | | Mol File: | 1496508-34-9.mol | ![Methanone, [(4aR)-1-(4-fluorophenyl)-1,4,5,6,7,8-hexahydro-6-[[4-(trifluoromethyl)phenyl]sulfonyl]-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl]-2-pyridinyl- Structure](CAS/20210305/GIF/1496508-34-9.gif) |
| | Methanone, [(4aR)-1-(4-fluorophenyl)-1,4,5,6,7,8-hexahydro-6-[[4-(trifluoromethyl)phenyl]sulfonyl]-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl]-2-pyridinyl- Chemical Properties |
| Boiling point | 692.9±65.0 °C(Predicted) | | density | 1.46±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | form | Solid | | pka | 3.35±0.10(Predicted) | | color | Off-white to light yellow |
| | Methanone, [(4aR)-1-(4-fluorophenyl)-1,4,5,6,7,8-hexahydro-6-[[4-(trifluoromethyl)phenyl]sulfonyl]-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl]-2-pyridinyl- Usage And Synthesis |
| Uses | Dazucorilant (CORT113176) is a selective and high affinity non-steroidal glucocorticoid receptor (GR) modulator with a Ki value ＜1 nM in vitro. Dazucorilant can be used for the research of neurological disorders[1][2]. | | in vivo | Dazucorilant (30 mg/kg/day; s.c.) makes mice show reversed abnormalities of motoneurons and down-regulated proinflammatory mediators and glial reactivity[1].
Dazucorilant (5, 10 or 20 mg/kg; i.p.) reverses hippocampal amyloid-β peptide generation, neuroinflammation and apoptotic processes, restores the hippocampal levels of synaptic markers, reestablishes basal plasma levels of glucocorticoids and improves cognitive function at a dose of 10 mg/kg[2]. | Animal Model: | Wobbler mice (five-month-old)[1] | | Dosage: | 30 mg/kg/day | | Administration: | S.c. | | Result: | Wobbler mice showed reversed abnormalities of motoneurons and down-regulated proinflammatory mediators and glial reactivity.
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| Animal Model: | Adult SD male rats[2] | | Dosage: | 5, 10 or 20 mg/kg | | Administration: | I.p. | | Result: | Reversed hippocampal amyloid-β peptide generation, neuroinflammation and apoptotic processes, restored the hippocampal levels of synaptic markers, reestablished basal plasma levels of glucocorticoids and improved cognitive function at a dose of 10 mg/kg.
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| | References | [1] Meyer M, et al. The Selective Glucocorticoid Receptor Modulator Cort 113176 Reduces Neurodegeneration and Neuroinflammation in Wobbler Mice Spinal Cord. Neuroscience. 2018;384:384-396. DOI:10.1016/j.neuroscience.2018.05.042
[2] Pineau F, et al. New selective glucocorticoid receptor modulators reverse amyloid-β peptide-induced hippocampus toxicity. Neurobiol Aging. 2016;45:109-122. DOI:10.1016/j.neurobiolaging.2016.05.018
[3] Canet G, et al. Central Role of Glucocorticoid Receptors in Alzheimer's Disease and Depression. Front Neurosci. 2018;12:739. Published 2018 Oct 16. DOI:10.3389/fnins.2018.00739 |
| | Methanone, [(4aR)-1-(4-fluorophenyl)-1,4,5,6,7,8-hexahydro-6-[[4-(trifluoromethyl)phenyl]sulfonyl]-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl]-2-pyridinyl- Preparation Products And Raw materials |
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