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CAS No. : 148451-96-1
MCE 国际站:L-732138
产品活性:L-732138 是一种选择性,有效和竞争性神经激肽-1 (NK-1) 受体拮抗剂,IC50 为 2.3 nM。L-732138 在克隆的人 NK-1 受体中的效力比在克隆大鼠 NK-1 受体中高 200 倍,比人类 NK-2 和 NK-3 受体高 1000 倍以上。L-732138 可减轻痛觉过敏并具有抗肿瘤作用。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:Neurokinin Receptor
In Vitro: 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.
In Vivo: 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.
相关产品:Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Neuronal Signaling Compound Library | Anti-Cancer Compound Library | Neurotransmitter Receptor Compound Library | Targeted Diversity Library | Antidepressant Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | Talnetant hydrochloride | [Tyr8,Nle11] Substance P | Neurokinin A(4-10) TFA | Maropitant-13C,d3 | [Sar4] Substance P (4-11) | MEN11467 | Spantide I TFA | [MePhe8,Sar9] Substance P | (β-Ala8)-Neurokinin A (4-10) | [MePhe7]-Neurokinin B | MLGFFQQPKPR-NH2 | Vapreotide acetate | Rolapitant | Biotin-NeurokininA | [D-Pro2,D-Trp7,9] Substance P | MEN 10207 | Ibodutant | Netupitant metabolite Monohydroxy Netupitant | Fezolinetant | SB-222200 | Neurokinin A TFA | Neurokinin B TFA | Septide | CS-003 Free base | Phyllomedusin | Imnopitant | Men 10376 TFA | [Lys5,MeLeu9,Nle10]-NKA(4-10) | Fosaprepitant dimeglumine
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货号: HY-101249
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