| Identification | Back Directory | [Name]
Methanone, [(4aR)-1-(4-fluorophenyl)-1,4,5,6,7,8-hexahydro-6-[(2-methyl-2H-1,2,3-triazol-4-yl)sulfonyl]-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl][4-(trifluoromethyl)-2-pyridinyl]- | [CAS]
1496509-78-4 | [Synonyms]
nonocorilant
Nenocorilant
Methanone, [(4aR)-1-(4-fluorophenyl)-1,4,5,6,7,8-hexahydro-6-[(2-methyl-2H-1,2,3-triazol-4-yl)sulfonyl]-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl][4-(trifluoromethyl)-2-pyridinyl]- | [Molecular Formula]
C26H21F4N7O3S | [MOL File]
1496509-78-4.mol | [Molecular Weight]
587.55 |
| Chemical Properties | Back Directory | [Boiling point ]
729.6±70.0 °C(Predicted) | [density ]
1.59±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
0.20±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Nenocorilantis a potent, orally activity glucocorticoid receptor (GR) antagonist with Ki value of 0.15 nM. Nenocorilant has pro-apoptotic effects and improves potency combined with cytotoxic agent. Nenocorilant can be used for cancer research[1][2][3]. | [in vivo]
Nenocorilant (30 mg/kg; p.o.; once every four days, for 25 d; female Balb/c nude mice) improves the efficacy and promotes apoptotic activity of cytotoxic therapy in xenograft models under physiological cortisol conditions[1]. | Animal Model: | Female Balb/c nude mice[1] | | Dosage: | 30 mg/kg | | Administration: | Oral administration; once every four days, for 25 days | | Result: | Inhibited tumor growth and increased the expression level of caspase 3. |
| [References]
[1] Greenstein AE, et, al. Glucocorticoid receptor antagonism promotes apoptosis in solid tumor cells. Oncotarget. 2021 Jun 22;12(13):1243-1255.
[2] Stringer-Reasor EM, et, al. Glucocorticoid receptor activation inhibits chemotherapy-induced cell death in high-grade serous ovarian carcinoma. Gynecol Oncol. 2015 Sep;138(3):656-62. DOI:10.1016/j.ygyno.2015.06.033
[3] WHO Drug Information. International Nonproprietary Names for Pharmaceutical |
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