中文名 | Irosustat |
英文名 | 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c][1]benzopyran-3-yl sulfaMate |
别名 | 化合物IROSUSTAT 6-氧代-6,7,8,9,10,11-六氢环庚并[C]苯并吡喃-3-基氨基磺酸酯 6-氧代-6,7,8,9,10,11-六氢环庚[C] [1]苯并吡喃-3-基磺酸盐 |
英文别名 | STX 64 BN 83495 Irosustat COUMATE. Irosustat. DSLPMJSGSBLWRE-UHFFFAOYSA-N 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-yl sulfamate 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c][1]benzopyran-3-yl sulfaMate |
CAS | 288628-05-7 |
EINECS | 604-604-1 |
化学式 | C14H15NO5S |
分子量 | 309.34 |
密度 | 1.48±0.1 g/cm3(Predicted) |
熔点 | 170.1-173.4 °C |
沸点 | 544.1±60.0 °C(Predicted) |
溶解度 | DMSO: >20 mg/mL |
酸度系数 | 8.26±0.70(Predicted) |
存储条件 | 2-8°C |
外观 | 白色粉末 |
体外研究 | Irosustat (667 COUMATE) is a potent steroid sulfatase inhibitor, with an IC 50 of 8 nM. Irosustat (667 COUMATE) inhibits steroid sulphatase (STS) activity in MCF-7 cells with an IC 50 of 0.2 nM, but has no effect on the morphology or proliferation of MCF-7 cells at 10 μM. |
体内研究 | Irosustat potently inhibits rat liver, with inhibition of >90% when at a 1 mg/kg concentration. Irosustat (2 mg/kg, p.o. for 5 d) blocks the uterine growth stimulated by oestrone sulfate (E1S) in ovariectomized rats. In addition, Irosustat (2, 10 mg/kg, p.o.) plus E1S dose-dependently decreases the growth of NMU-induced mammary tumors in ovariectomized rats. Irosustat (667 COUMATE; 10 mg/kg, p.o.) shows 97.9 ± 0.06% inhibition on steroid sulphatase (STS) activity in rat liver. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.233 ml | 16.164 ml | 32.327 ml |
5 mM | 0.647 ml | 3.233 ml | 6.465 ml |
10 mM | 0.323 ml | 1.616 ml | 3.233 ml |
5 mM | 0.065 ml | 0.323 ml | 0.647 ml |
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