21715-46-8
中文名稱
艾替伏辛
英文名稱
Etifoxine
CAS
21715-46-8
分子式
C17H17ClN2O
分子量
300.78
MOL 文件
21715-46-8.mol
更新日期
2024/11/15 18:20:34
21715-46-8 結(jié)構(gòu)式
基本信息
中文別名
艾替伏辛2-乙基氨基-6-氯-4-甲基-4-苯基-4H-3,1-苯并惡嗪
英文別名
36-801Etifoxin
Etifoxine
HOE-36801
HOE-36-801
etafenoxine
2-Ethylamino-6-chloro-4-methyl-4-phenyl-4H-3,1-benzoxazine
6-Chloro-2-ethylamino-4-methyl-4-phenyl-4H-3,1-benzoxazine
4H-3,1-Benzoxazin-2-amine, 6-chloro-N-ethyl-4-methyl-4-phenyl-
物理化學(xué)性質(zhì)
熔點(diǎn)90-92℃
沸點(diǎn)421.2±55.0 °C(Predicted)
密度1.1716 (rough estimate)
蒸氣壓0-1Pa at 20-25℃
折射率1.5800 (estimate)
儲存條件-20°C儲存
溶解度DMSO:60.0(Max Conc. mg/mL);199.47(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);99.74(Max Conc. mM)
DMF:PBS (pH 7.2) (1:8):0.1(Max Conc. mg/mL);0.33(Max Conc. mM)
Ethanol:20.0(Max Conc. mg/mL);66.49(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);99.74(Max Conc. mM)
DMF:PBS (pH 7.2) (1:8):0.1(Max Conc. mg/mL);0.33(Max Conc. mM)
Ethanol:20.0(Max Conc. mg/mL);66.49(Max Conc. mM)
酸度系數(shù)(pKa)4.89±0.40(Predicted)
形態(tài)固體：顆粒/粉末
顏色Light yellow to yellow
LogP4.09-4.52 at 21-25℃ and pH7
艾替伏辛價(jià)格(試劑級)
| 報(bào)價(jià)日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價(jià)格 |
| 2024/11/08 | HY-16579A | 艾替伏辛 Etifoxine | 21715-46-8 | 5mg | 780元 |
| 2024/11/08 | HY-16579A | 艾替伏辛 Etifoxine | 21715-46-8 | 10mM * 1mLin DMSO | 858元 |
| 2024/11/08 | HY-16579A | 艾替伏辛 Etifoxine | 21715-46-8 | 10mg | 1100元 |
常見問題列表
生物活性
Etifoxine 是一個(gè)非苯二氮卓類的、具有 GABA 能的化合物，是 GABAA 受體亞基 α1β2γ2 和 α1β3γ2 的陽性變構(gòu)調(diào)節(jié)劑。Etifoxine 在嚙齒類動物中顯示出抗焦慮和抗驚厥活性。體外研究
Etifoxine (EFX), at concentrations ranging from 10 to 300 μM (higher concentrations limited its solubility), produces a dose-dependent increase in the [3H]muscimol binding at equilibrium, to 155±2% of its control value at 300 μM EFX.
體內(nèi)研究
Etifoxine competitively inhibits [
35
S]TBPS binding with micromolar potency in rat brain.
Etifoxine (3.125-50 mg/kg) exhibits more pronounced anxiolytic and anticonvulsant effects in the BALB/cByJ mice compared to the C57BL/6J mice.
| Animal Model: | Six-week old BALB/cByJ and C57BL/6J mice (20-25 g). |
| Dosage: | 3.125-50 mg/kg. |
| Administration: | Intraperitoneal injection. |
| Result: |
Significantly increased the amount of time spent on the open arms at the 12.5 mg/kg dose when compared to vehicle (p = 0.009) in BALB/cByJ mice but produced no effect in C57B/6J mice.
BALB/cByJ mice compared with C57BL/6J mice exhibited significantly (p < 0.012) lower plasma levels of the compound at 15 and 30 min. |