L732138
| 中文名称 | L732138 |
|---|---|
| 中文同义词 | N-乙酰基-L-色氨酸-3,5-双(三氟甲基)苯酯;(S)-3,5-双(三氟甲基)苄基 2-乙酰氨基-3-(1H-吲哚-3-基)丙酸酯;化合物L-732138;L-732,138,NK1拮抗剂 |
| 英文名称 | AC-TRP-3,5-BIS(TRIFLUOROMETHYL)BENZYL ESTER |
| 英文同义词 | N-ACETYL-L-TRYPTOPHAN 3,5-BIS(TRIFLUOROMETHYL)-BENZYL ESTER;L-732,138;AC-TRP-3,5-BIS(TRIFLUOROMETHYL)BENZYL ESTER;N-acetyl-L-tryptophan 3,5-bis*(trifluoromethyl)be;L732138;N-ACETYL-L-TRYPTOPHAN 3,5-BIS(TRIFLUOROM ETHYL)BENZ;3,5-bis(trifluoromethyl)benzyl N-acetyltryptophan;N-Acetyl-L-tryptophan 3,5-bis(trifluoromethyl)benzyl ester,L-732,138 |
| CAS号 | 148451-96-1 |
| 分子式 | C22H18F6N2O3 |
| 分子量 | 472.38 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 148451-96-1.mol |
| 结构式 |  |
L732138 性质
| 熔点 | 147-148 °C(lit.) |
|---|---|
| 沸点 | 554.1±50.0 °C(Predicted) |
| 密度 | 1.396±0.06 g/cm3(Predicted) |
| 储存条件 | Sealed in dry,Store in freezer, under -20°C |
| 溶解度 | 在乙醇中溶解度为 100 mM，在 DMSO 中溶解度为 100 mM |
| 酸度系数(pKa) | 14.63±0.46(Predicted) |
| 形态 | 粉末 |
| Target | Value |
|
NK-1 receptor
(in CHO cells) | 2.3 nM |
L-732138 (0 -100 µM; first doubling time; COLO 858, MEL HO and COLO 679 cells) treatment results in a concentration-dependent cytotoxicity. L-732138 inhibits cell growth with IC
50
of 44.6 μM for COLO 858 cells, 76.3 μM for MEL HO cells and 64.2 μM for COLO 679 cells. L-732138 blocks substance P (SP) mitogen stimulation.
L-732,138 treatment results in a large number of apoptotic cells were found in COLO 858, MEL HO and COLO 679 melanoma cell lines. In DAPI-stained cultures, at IC
50
concentration of 43.6% apoptotic cells for the three melanoma cell lines, whereas at IC
100
concentration of 51.4 % apoptotic cells.
Cell Proliferation Assay
| Cell Line: | COLO 858, MEL HO and COLO 679 cells |
| Concentration: | 0 µM, 20 µM, 40 µM, 60 µM, 80 µM, 100 µM |
| Incubation Time: | First doubling time |
| Result: | Resulted in a concentration-dependent cytotoxicity. |
L-732138 (10 -4 -10 -2 mol/kg; intravenous injection; for 15 minutes; male Dunkin-Hartley guinea-pigs) treatment abolishes vagally-induced plasma exudation and significantly inhibits the enhancement by LPS. The LPS-enhanced vagally-induced plasma exudation is not completely inhibited by either L-732138 or SOD pretreatment alone, but is blocked by the combination of both pretreatments.
| Animal Model: | Male Dunkin-Hartley guinea-pigs (350-500 g) injected with lipopolysaccharide (LPS) |
| Dosage: | 10 -4 mol/kg , 10 -3 mol/kg and 10 -2 mol/kg |
| Administration: | Intravenous injection; for 15 minutes |
| Result: | Abolished the vagally-induced plasma leakage in tracheobronchial tissues, and dose-dependently inhibited the LPS enhanced vagally-induced plasma exudation in traceobronchial tissues. |
安全信息
| WGK Germany | 3 |
|---|
| 提供商 | 语言 |
|---|---|
|
英文
|
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-101249 | L732138 L-732138 | 148451-96-1 | 5mg | 2200元 |
| 2024/04/30 | HY-101249 | L732138 L-732138 | 148451-96-1 | 10mM * 1mLin DMSO | 2420元 |