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188116-07-6

中文名稱 伊匹妥英
英文名稱 1-(4-chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one
CAS 188116-07-6
分子式 C13H14ClN3O2
分子量 279.72
MOL 文件 188116-07-6.mol
更新日期 2025/01/10 15:39:04
188116-07-6 結(jié)構(gòu)式 188116-07-6 結(jié)構(gòu)式

基本信息

中文別名
伊匹妥英
1-(4-氯苯基)-1,5-二氫-4-(4-嗎啉基)-2H-咪唑-2-酮
英文別名
CS-1057
ELB-138
Imepitoin
AWD 131-13
AWD 131-138, >=98%
IMEPITOIN
AWD131-138
AWD 131-138(Imepitoin)
3-(4-chlorophenyl)-5-morpholin-4-yl-4H-imidazol-2-one
1-(4-chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one
1-(4-CHLOROPHENYL)-4-MORPHOLINO-1H-IMIDAZOL-2(5H)-ONE

物理化學(xué)性質(zhì)

熔點264℃ (ethanol )
沸點421.8±55.0 °C(Predicted)
密度1.42±0.1 g/cm3(Predicted)
儲存條件Sealed in dry,2-8°C
溶解度DMF:10.0(Max Conc. mg/mL);35.75(Max Conc. mM)
DMSO:17.5(Max Conc. mg/mL);62.56(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.79(Max Conc. mM)
Ethanol:1.13(Max Conc. mg/mL);4.02(Max Conc. mM)
酸度系數(shù)(pKa)4.39±0.20(Predicted)
形態(tài)A crystalline solid
顏色White to off-white

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS08
警示詞警告
危險性描述H361d
伊匹妥英價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-14953伊匹妥英
Imepitoin
188116-07-65mg545元
2024/11/08HY-14953伊匹妥英
Imepitoin
188116-07-610mM * 1mLin DMSO599元
2024/11/08HY-14953伊匹妥英
Imepitoin
188116-07-610mg885元

常見問題列表

生物活性
Imepitoin (AWD 131-138) 是低親和力的部分苯二氮(benzodiazepine)受體激動劑,有抗痙攣和抗焦慮作用。
靶點

GABA receptor

體外研究

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].

體內(nèi)研究

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].

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