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-
![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)
- CAS No.
- 1496508-34-9
- Chemical 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
- CORT113176;Dazucorilant;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-
- CBNumber:
- CB99807357
- Molecular Formula:
- C29H22F4N4O3S
- Molecular Weight:
- 582.57
- MDL Number:
- 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- 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 |
| FDA UNII | HR4RD5RBJ6 |
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,Uses,Production
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. |
| 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. |
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
Raw materials
Preparation Products
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- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Chunchuang (Wuhan) Technology Co., Ltd | 15727060112 | yutianchun2007@126.com | China | 10000 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24844 | 58 |
| Nantong QuanYi Biotechnology Co., Ltd | 0513-66337626 18051384581 | sales@chemhifuture.com | China | 5300 | 58 |
| Supplier | Advantage |
|---|---|
| Chunchuang (Wuhan) Technology Co., Ltd | 58 |
| TargetMol Chemicals Inc. | 58 |
| Nantong QuanYi Biotechnology Co., Ltd | 58 |