|
|
| | 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]- Basic information |
| Product 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]- | | Synonyms: | 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]-;nonocorilant;Nenocorilant | | CAS: | 1496509-78-4 | | MF: | C26H21F4N7O3S | | MW: | 587.55 | | EINECS: | | | Product Categories: | | | Mol File: | 1496509-78-4.mol | ![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]- Structure](CAS/20210305/GIF/1496509-78-4.gif) |
| | 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]- Chemical Properties |
| Boiling point | 729.6±70.0 °C(Predicted) | | density | 1.59±0.1 g/cm3(Predicted) | | pka | 0.20±0.40(Predicted) | | form | Solid | | color | White to off-white |
| | 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]- Usage And Synthesis |
| 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 |
| | 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]- Preparation Products And Raw materials |
|