L-732138

Research use only, not for human use.

L-732138 is a potent and competitive antagonist of neurokinin-1 (NK-1) receptor(IC50 : 2.3 nM).

L-732138 is a potent and competitive antagonist of neurokinin-1 (NK-1) receptor(IC50 : 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 IC50 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 IC50 concentration of 43.6% apoptotic cells for the three melanoma cell lines, whereas at IC100 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 withlipopolysaccharide (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.

——

GPCR/G Protein

Neurokinin Receptor

NK-1

——

——

148451-96-1

472.38

C22H18F6N2O3

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (529.23 mM)

CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(cc(c1)C(F)(F)F)C(F)(F)F

[35-Bis(trifluoromethyl)phenyl]methyl (2S)-2-acetamido-3-(1H-indol-3-yl)propanoate

(-20℃)

With Ice Pack

≥ 2 years