| Identification | Back Directory | [Name]
2,2-difluoro-N-((1R,2S)-3-methyl-1-((1-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-1H-indazol-5-yl)oxy)-1-phenylbutan-2-yl)propanamide | [CAS]
1893415-00-3 | [Synonyms]
EOS-61736
mizacorat
2,2-difluoro-N-((1R,2S)-3-methyl-1-((1-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-1H-indazol-5-yl)oxy)-1-phenylbutan-2-yl)propanamide
Propanamide, N-[(1S)-1-[(R)-[[1-(1,6-dihydro-1-methyl-6-oxo-3-pyridinyl)-1H-indazol-5-yl]oxy]phenylmethyl]-2-methylpropyl]-2,2-difluoro- | [Molecular Formula]
C27H28F2N4O3 | [MDL Number]
MFCD31619227 | [MOL File]
1893415-00-3.mol | [Molecular Weight]
494.53 |
| Chemical Properties | Back Directory | [Boiling point ]
629.3±55.0 °C(Predicted) | [density ]
1.26±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
12.93±0.46(Predicted) | [color ]
Off-white to light brown | [Water Solubility ]
Water : < 0.1 mg/mL (insoluble) |
| Hazard Information | Back Directory | [Uses]
Mizacorat (AZD9567; compound 15) is a potent, oral active, non-steroidal and selective glucocorticoid receptor modulator (SGRM), with an IC50 of 3.8 nM. Exhibits excellent efficacy in the streptococcal cell wall (SCW) reactivation model of joint inflammation[1]. | [in vivo]
Mizacorat (15 mg/kg/day, Oral gavage daily for 8 days) treatment shows excellent in vivo efficacy in a rat model of joint inflammation[1]. | Animal Model: | Antigen-induced joint inflammation model in female Lewis rats (175-200 g), sensitized by an intra-articular injection of 5 μg of SCW[1]. | | Dosage: | 15 mg/kg/day. | | Administration: | Oral gavage daily for 8 days. | | Result: | Inhibited ankle swelling in the rat SCW model. |
| [storage]
Store at -20°C | [References]
[1] Ripa L, et al. Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile. J Med Chem. 2018 Mar 8;61(5):1785-1799. DOI:10.1021/acs.jmedchem.7b01690 |
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