溴米索伐
中文名称 | 溴米索伐 |
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中文同义词 | α-溴代异戊酰脲;布洛母拉;溴米那;溴米那 1G;溴米索伐;溴米索伐(溴米那);溴异戊脲;α-溴异戊酰脲 |
英文名称 | Bromisoval |
英文同义词 | RARECHEM AX KI 5046;1-(2-BROMOISOVALERYL)UREA;A-(BROMOISOVALERYL)UREA;ALPHA(BROMOISOVALERYL)UREA;LABOTEST-BB LT00134620;BROMOVALERYLUREA;BROMOISOVALERYLUREA;BROMO-ISO-VALERYLUREA (ALPHA) |
CAS号 | 496-67-3 |
分子式 | C6H11BrN2O2 |
分子量 | 223.07 |
EINECS号 | 207-825-7 |
相关类别 | 医药中间体;脲;小分子抑制剂;医药原料;镇静催眠药;其他原料药;医药、农药及染料中间体;API |
Mol文件 | 496-67-3.mol |
结构式 |
溴米索伐 性质
熔点 | 152 °C |
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密度 | 1.6005 (rough estimate) |
折射率 | 1.5410 (estimate) |
储存条件 | Sealed in dry,Room Temperature |
溶解度 | 可溶于DMSO(少许)、甲醇(少许) |
形态 | 固体 |
酸度系数(pKa) | 10.54±0.70(Predicted) |
颜色 | 白色至类白色 |
水溶解性 | 19.03g/L(temperature not stated) |
Merck | 14,1397 |
InChIKey | CMCCHHWTTBEZNM-UHFFFAOYSA-N |
CAS 数据库 | 496-67-3(CAS DataBase Reference) |
NIST化学物质信息 | Bromisovalum(496-67-3) |
EPA化学物质信息 | Butanamide, N-(aminocarbonyl)-2-bromo-3-methyl- (496-67-3) |
Bromisoval (BU) suppresses nitric oxide (NO) releasing and proinflammatory cytokine expression in lipopolysaccharide (LPS)-treat BV2 cells, a murine microglial cell line. Bromisoval suppresses LPS-inducing phosphorylation of signal transducer and activator of transcription 1 (STAT1) and expression of interferon regulatory factor 1 (IRF1). The Janus kinase 1 (JAK1) inhibitor filgotinib suppresses the NO release much more weakly than that of Bromisoval, although filgotinib almost completely prevents LPS-inducing STAT1 phosphorylation. Knockdown of JAK1, STAT1, or IRF1 does not affect the suppressive effects of Bromisoval on LPS-inducing NO. A combination of Bromisoval and filgotinib synergistically suppress the NO releasing. The mitochondrial complex I inhibitor rotenone, which does not prevent STAT1 phosphorylation or IRF1 expression, suppresses proinflammatory mediator expression less significantly than Bromisoval. Bromisoval and rotenone reduce intracellular ATP (iATP) levels to a similar extent. A combination of rotenone and filgotinib suppress NO release in LPS-treated BV2 cells as strongly as Bromisoval.
Bromisoval (Bromvaletone) and carbromal are the most potent central depressants within each series. Depressant activities (ISD 50 values) and acute toxicities (LD 50 values) in male mice after intraperitoneal injection of Bromisoval are 0.35 (0.30-0.39) and 3.25 (2.89-3.62) mmol/kg, respectively.
安全信息
RTECS号 | YS3150000 |
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海关编码 | 2924.19.8000 |
毒性 | LD50 in male mice (mmoles/kg): 3.25 i.p. (Mrongovius) |