Name | N-acetyl-L-tryptophan 3,5-bis*(trifluoromethyl)be |
Synonyms | L732138 L-732,138 AC-TRP-3,5-BIS(TRIFLUOROMETHYL)BENZYL ESTER 3,5-bis(trifluoromethyl)benzyl N-acetyltryptophan N-acetyl-L-tryptophan 3,5-bis*(trifluoromethyl)be 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 |
CAS | 148451-96-1 |
InChI | InChI=1/C22H18F6N2O3/c1-12(31)30-19(8-14-10-29-18-5-3-2-4-17(14)18)20(32)33-11-13-6-15(21(23,24)25)9-16(7-13)22(26,27)28/h2-7,9-10,19,29H,8,11H2,1H3,(H,30,31)/t19-/m0/s1 |
Molecular Formula | C22H18F6N2O3 |
Molar Mass | 472.38 |
Density | 1.396±0.06 g/cm3(Predicted) |
Melting Point | 147-148°C(lit.) |
Boling Point | 554.1±50.0 °C(Predicted) |
Flash Point | 288.9°C |
Vapor Presure | 2.56E-12mmHg at 25°C |
Appearance | powder |
pKa | 14.63±0.46(Predicted) |
Storage Condition | Sealed in dry,Store in freezer, under -20°C |
Refractive Index | 1.541 |
WGK Germany | 3 |
biological activity | L-732138 (L-732,138) is an effective and selective competitive antagonist of neurokinin-1 (NK-1) receptor/substance P (SP) receptor. L-732138 inhibited the binding of 125I-SP to stably expressed human NK-1 receptors in CHO cells with an IC50 value of 2.3 nM. |
Target | Value |
NK-1 receptor (in CHO cells) | 2.3 nM |
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. Abolished the vagally-induced plasma leakage in tracheobronchial tissues, and dose-dependently inhibited the LPS enhanced vagally-induced plasma exudation in traceobronchial tissues. |
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 |