L732138
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- CAS号:
- 148451-96-1
- 英文名:
- AC-TRP-3,5-BIS(TRIFLUOROMETHYL)BENZYL ESTER
- 英文别名:
- L732138;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;3,5-Bis(trifluoromethyl)benzyl acetyl-L-tryptophanate;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
- 中文名:
- L732138
- 中文别名:
- 化合物L-732138;L-732,138,NK1拮抗剂;N-乙酰基-L-色氨酸-3,5-双(三氟甲基)苯酯;(S)-3,5-双(三氟甲基)苄基 2-乙酰氨基-3-(1H-吲哚-3-基)丙酸酯
- CBNumber:
- CB1721780
- 分子式:
- C22H18F6N2O3
- 分子量:
- 472.38
- MOL File:
- 148451-96-1.mol
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L732138化学性质
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熔点:
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147-148 °C(lit.)
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沸点:
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554.1±50.0 °C(Predicted)
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密度:
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1.396±0.06 g/cm3(Predicted)
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储存条件:
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Sealed in dry,Store in freezer, under -20°C
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溶解度:
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Soluble to 100 mM in ethanol and to 100 mM in DMSO
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酸度系数(pKa):
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14.63±0.46(Predicted)
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形态:
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powder
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颜色:
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White to off-white
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L732138性质、用途与生产工艺
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。
| Target | Value |
NK-1 receptor
(in CHO cells)
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2.3 nM
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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
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Cell Line:
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COLO 858, MEL HO and COLO 679 cells
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Concentration:
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0 µM, 20 µM, 40 µM, 60 µM, 80 µM, 100 µM
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Incubation Time:
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First doubling time
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Result:
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Resulted in a concentration-dependent cytotoxicity.
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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.
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Animal Model:
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Male Dunkin-Hartley guinea-pigs (350-500 g) injected with lipopolysaccharide (LPS)
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Dosage:
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10
-4
mol/kg , 10
-3
mol/kg and 10
-2
mol/kg
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Administration:
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Intravenous injection; for 15 minutes
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Result:
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Abolished the vagally-induced plasma leakage in tracheobronchial tissues, and dose-dependently inhibited the LPS enhanced vagally-induced plasma exudation in traceobronchial tissues.
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L732138
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/11/08 | HY-101249 | L732138
L-732138 | 148451-96-1 | 5mg | 2200元 |
| 2024/11/08 | HY-101249 | L732138
L-732138 | 148451-96-1 | 10mM * 1mLin DMSO | 2420元 |
148451-96-1, L732138 相关搜索:
- 抑制剂
- 合成有机化合物配体
- Peptides
- Tachykinins
- Antagonist
- Biochemicals and Reagents
- BioChemical
- Amino Acids and Peptides
- C22H18F6N2O3
- L-732,138,NK1拮抗剂
- 化合物L-732138
- (S)-3,5-双(三氟甲基)苄基 2-乙酰氨基-3-(1H-吲哚-3-基)丙酸酯
- N-乙酰基-L-色氨酸-3,5-双(三氟甲基)苯酯
- 148451-96-1
- cytotoxicity,vagally-induced,NK receptor,Neurokinin Receptor,Inhibitor,ntravenously,lipopolysaccharide,plasma,Tachykinin receptor,stimulation,L732138,mitogen,peralgesia,inhibit,L-732138,Antitumorhy,apoptotic,L 732138
- 3,5-Bis(trifluoromethyl)benzyl acetyl-L-tryptophanate
- N-Acetyl-L-tryptophan 3,5-bis(trifluoromethyl)benzyl ester >=99% (TLC), powder
- L-Tryptophan, N-acetyl-, [3,5-bis(trifluoromethyl)phenyl]methyl ester
- [3,5-Bis(Trifluoromethyl)phenyl]methyl (2S)-2-acetamido-3-(1H-Indol-3-Yl)propanoate
- N-Acetyl-L-tryptophan 3,5-bis(trifluoromethyl)benzyl ester,L-732,138
- 3,5-bis(trifluoromethyl)benzyl N-acetyltryptophan
- N-ACETYL-L-TRYPTOPHAN 3,5-BIS(TRIFLUOROM ETHYL)BENZ
- L732138
- N-acetyl-L-tryptophan 3,5-bis*(trifluoromethyl)be
- AC-TRP-3,5-BIS(TRIFLUOROMETHYL)BENZYL ESTER
- L-732,138
- N-ACETYL-L-TRYPTOPHAN 3,5-BIS(TRIFLUOROMETHYL)-BENZYL ESTER