L732138

生物活性靶点体外研究体内研究 L732138 试剂级价格

L732138

CAS号:148451-96-1
英文名:AC-TRP-3,5-BIS(TRIFLUOROMETHYL)BENZYL ESTER
中文名:L732138
CBNumber:CB1721780
分子式:C22H18F6N2O3
分子量:472.38
MOL File:148451-96-1.mol

L732138化学性质

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 :Soluble to 100 mM in ethanol and to 100 mM in DMSO
酸度系数(pKa) :14.63±0.46(Predicted)
形态 :powder
颜色 :White to off-white

安全信息

WGK Germany :3

L732138性质、用途与生产工艺

生物活性 L-732138 (L-732,138) 是一种有效的、选择性的 neurokinin-1 (NK-1) receptor/substance P (SP) receptor 的竞争性拮抗剂。L-732138 可在CHO细胞中抑制125I-SP与稳定表达的人类NK-1受体的结合，其IC50值为2.3 nM。
靶点
Target Value
NK-1 receptor
(in CHO cells) 2.3 nM

体外研究

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.

体内研究

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.