- Imepitoin
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- $35.00
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2026-04-22
- CAS:188116-07-6
- Purity: 99.82%
- Supply Ability: 10g
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| | 1-(4-chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one Basic information |
| Product Name: | 1-(4-chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one | | Synonyms: | 1-(4-chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one;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%;IMEPITOIN; AWD131-138;CS-1057 | | CAS: | 188116-07-6 | | MF: | C13H14ClN3O2 | | MW: | 279.72 | | EINECS: | 200-256-5 | | Product Categories: | Inhibitors | | Mol File: | 188116-07-6.mol |  |
| | 1-(4-chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one Chemical Properties |
| Melting point | 264℃ (ethanol ) | | Boiling point | 421.8±55.0 °C(Predicted) | | density | 1.42±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | 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) | | form | A crystalline solid | | pka | 4.39±0.20(Predicted) | | color | White to off-white |
| | 1-(4-chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one Usage And Synthesis |
| Uses | 1-(4-Chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-2H-imidazol-2-one is used in treating feline epilepsy. | | Biological Activity | Imepitoin (AWD 131-138; ELB 138) is a g-aminobutyric acid A (GABAA) receptor partial positive allosteric modulator (PAM) th at targets the benzodiazepine (BZD)-binding site at the α/γ2-interface. Imepitoin enhances GABA current (% response/[GABA] alone in μM/receptor complex = 320/3/α1β2γ2, 310/25/α1β3γ2, 460/8/α2β2γ2, 590/12/α3β2γ2 and 290/3/α5β2γ2 using Xenopus oocytes expressing respective r at receptor complex) with ~2% the potency and 17-27% the efficacy of diazepam toward α1β2γ2. Imepitoin exhibits in vivo therapeutic efficacy in animal models of seizure and epilepsy. | | in vivo | 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]. |
| | 1-(4-chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one Preparation Products And Raw materials |
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