伊匹妥英
中文名称 | 伊匹妥英 |
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中文同义词 | 伊匹妥英;1-(4-氯苯基)-1,5-二氢-4-(4-吗啉基)-2H-咪唑-2-酮;1-(4-氯苯基)-4-吗啉-1H-咪唑-2(5H)-酮;异匹妥因;优选]AWD 131-138 |
英文名称 | 1-(4-chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one |
英文同义词 | 1-(4-chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one;Imepitoin;1-(4-CHLOROPHENYL)-4-MORPHOLINO-1H-IMIDAZOL-2(5H)-ONE;1-(4-Chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-2H-imidazol-2-one;2H-Imidazol-2-one,1-(4-chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-;Imepitoin 1-(4-Chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-2H-imidazol-2-one;AWD 131-138, >=98%;3-(4-chlorophenyl)-5-morpholin-4-yl-4H-imidazol-2-one |
CAS号 | 188116-07-6 |
分子式 | C13H14ClN3O2 |
分子量 | 279.72 |
EINECS号 | 200-256-5 |
相关类别 | 小分子抑制剂;小分子抑制剂,天然产物;原料药及中间体;化学试剂;Inhibitors |
Mol文件 | 188116-07-6.mol |
结构式 |
伊匹妥英 性质
熔点 | 264℃ (ethanol ) |
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沸点 | 421.8±55.0 °C(Predicted) |
密度 | 1.42±0.1 g/cm3(Predicted) |
储存条件 | 2-8°C |
溶解度 | DMF:10.0(最大浓度 mg/mL);35.75(最大浓度 mM) DMSO:17.5(最大浓度 mg/mL);62.56(最大浓度 mM) DMSO:PBS ( pH 7.2) (1:1):0.5(最大浓度 mg/mL);1.79(最大浓度 mM) 乙醇:1.13(最大浓度 mg/mL);4.02(最大浓度 mM) |
形态 | 结晶固体 |
酸度系数(pKa) | 4.39±0.20(Predicted) |
GABA receptor
AWD 131-138 dose-dependently stimulated GABA currents(Recombinant gamma-aminobutyric acid A (GABA(A)) receptors of the subunit compositions alpha1beta2gamma2, alpha1beta3gamma2, alpha2beta2gamma2, alpha3beta2gamma2 and alpha5beta2gamma2). At 10 microM AWD 131-138, this allosteric stimulation amounted in average to about 12-21% of the maximal stimulation achieved using diazepam. The threshold of stimulation was about 0.3-1.0 microM [1].
AWD 131-138 did not produce midazolam-like responding or alter response rates at cumulative doses up to 18.0 mg/kg i.m. (plasma levels over 2100 ng/ml). When AWD 131-138 (10-100 microg/kg/injection) was studied by substitution, responding declined to vehicle substitution levels within three sessions. At the dose of 100 microg/kg i.v. AWD 131-138, sufficient drug was self-administered during the first session (about 3.5 mg/kg) to produce plasma levels above 1000 ng/ml, yet responding over the next two sessions dropped to vehicle levels [2]. Prolonged oral administration with twice-daily dosing of ELB 138 with either 5 or 40 mg/kg over a 5-week period was not associated with loss of anticonvulsant efficacy in the PTZ dog model [3].
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/01/25 | HY-14953 | 伊匹妥英 Imepitoin | 188116-07-6 | 5mg | 800元 |
2024/01/25 | HY-14953 | 伊匹妥英 Imepitoin | 188116-07-6 | 10mM * 1mLin DMSO | 880元 |