148451-96-1
148451-96-1 結(jié)構(gòu)式
基本信息
L-732,138
AC-TRP-3,5-BIS(TRIFLUOROMETHYL)BENZYL ESTER
N-acetyl-L-tryptophan 3,5-bis*(trifluoromethyl)be
3,5-bis(trifluoromethyl)benzyl N-acetyltryptophan
N-ACETYL-L-TRYPTOPHAN 3,5-BIS(TRIFLUOROM ETHYL)BENZ
N-ACETYL-L-TRYPTOPHAN 3,5-BIS(TRIFLUOROMETHYL)-BENZYL ESTER
N-Acetyl-L-tryptophan 3,5-bis(trifluoromethyl)benzyl ester,L-732,138
L-Tryptophan, N-acetyl-, [3,5-bis(trifluoromethyl)phenyl]methyl ester
N-Acetyl-L-tryptophan 3,5-bis(trifluoromethyl)benzyl ester >=99% (TLC), powder
物理化學(xué)性質(zhì)
常見問題列表
| 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. |