| Identification | Back Directory | [Name]
Benzenesulfonamide, N-(1-benzoyl-1,2,3,4-tetrahydro-6-quinolinyl)-5-chloro-2-methoxy-4-methyl- | [CAS]
2868357-11-1 | [Synonyms]
Benzenesulfonamide, N-(1-benzoyl-1,2,3,4-tetrahydro-6-quinolinyl)-5-chloro-2-methoxy-4-methyl- | [Molecular Formula]
C24H23ClN2O4S | [MOL File]
2868357-11-1.mol | [Molecular Weight]
470.97 |
| Chemical Properties | Back Directory | [Boiling point ]
665.2±65.0 °C(Predicted) | [density ]
1.362±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
8.80±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Glucocorticoid receptor modulator 1 is a highly potent and orally active non-steroidal selective glucocorticoid receptor modulator with an IC50 value of 9 nM and 130 nM for NF-κB and AP-1, respectively. Glucocorticoid receptor modulator 1 can effectively reduce the expression of inflammatory factors IL-6, IL-1β, TNF-α, also can relieve dermatitis in mice[1]. | [in vivo]
Glucocorticoid receptor modulator 1 (5, 10 and 20 mg/kg; p.o.; for 24 days) relieves dermatitis in mice and suppresses the expression of inflammatory factors[1]. | Animal Model: | Female BALB/C mice (5 weeks; 2,4-dinitrochlorobenzene-induced atopic dermatitis model)[1] | | Dosage: | 5, 10 and 20 mg/kg | | Administration: | p.o.; for 24 days | | Result: | Significantly improved the skin damage in a dose-dependent manner, and suppressed inflammatory factors of IL-6, IL-1β, TSLP, and MMP-13. |
| [References]
[1] Li D, Hou T, et al. Discovery and Optimization of N-Acyl-6-sulfonamide-tetrahydroquinoline Derivatives as Novel Non-Steroidal Selective Glucocorticoid Receptor Modulators. J Med Chem. 2022 Nov 18. DOI:10.1021/acs.jmedchem.2c01082 |
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