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
- 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
- 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。
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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.
- 更新日期：2024/11/08
- 产品编号：HY-101249
- 产品名称：L732138 L-732138
- CAS编号：148451-96-1
- 包装：5mg
- 价格：2200元
- 更新日期：2024/11/08
- 产品编号：HY-101249
- 产品名称：L732138 L-732138
- CAS编号：148451-96-1
- 包装：10mM * 1mLin DMSO
- 价格：2420元
- 公司名称：Bachem AG
- 联系电话：--
- 电子邮件：bachem.sale@yahoo.com
- 国家：瑞士
- 产品数：291
- 优势度：81
- 公司名称：SIGMA
- 联系电话：--
- 电子邮件：
- 国家：瑞士
- 产品数：6896
- 优势度：91
