Vapreotide acetate 产品活性：Vapreotide acetate (RC-160 acetate; BMY-41606 acetate) 是 神经激肽-1 (NK1) 受体拮抗剂，其 IC50 值为 330 nM。 产品来源： https://www.medchemexpress.cn/Vapreotide__acetate_.html 研究领域：GPCR/G Protein | Neuronal Signaling 作用靶点：Neurokinin Receptor In Vitro: Vapreotide attenuates the Substance P (SP)-triggered intracellular calcium increases and NF-κB activation in a dose-dependent manner. Vapreotide also inhibits SP-induced IL-8 and MCP-1 production in HEK293-NK1R and U373MG cell lines. Vapreotide inhibits HIV-1 infection of human MDM in vitro, an effect that is reversible by SP pretreatment. Vapreotide significantly inhibits GH-, PRL, and/or alpha-subunit release by human GH-secreting pituitary adenoma cells in concentrations as low as 10-12-10-14 M. Vapreotide inhibits GH release with an IC50 of 0.1 pM. Vapreotide exhibits moderate-to-high affinities for SSTR2, -3, and -5 (IC50=0.17, 0.1 and 21 nM, respectively) and low affinity for SSTR1 and -4 (IC50=200 and 620 nM, respectively). RC-160 inhibits serum-induced proliferation of CHO cells expressing SSTR2 and SSTR5 (EC50=53 and 150 pM, respectively). In Vivo: In cirrhosis, bleeding by rupture of oesophagogastric varices is a severe complication of portal hypertension. The acute administration of vapreotide to rats decreases collateral circulation blood flow while chronic administration attenuated its development. Tumor volumes and weights are reduced by about 40% by RC-160 by s.c. injections at doses of 100 μg/day/animal. Vapreotide can inhibit the growth of androgen-independent prostate cancer when the therapy is started at an early stage of tumor development. 相关产品：Drug Repurposing Compound Library Plus | FDA-Approved Drug Library Plus | Bioactive Compound Library Plus | Peptidomimetic Library | Macrocyclic Compound Library | Peptide Library | Substance P | Aprepitant | Fezolinetant | Senktide | Fosaprepitant dimeglumine | Netupitant | SB-222200 | Rolapitant | Saredutant | Talnetant | Maropitant | Casopitant mesylate | L-732138 | Elinzanetant | H-Glu(OtBu)-OtBu hydrochloride | Neurokinin A TFA | Vofopitant dihydrochloride | Osanetant | Neurokinin B TFA | Pavinetant | Substance P(1-7) TFA | Hemokinin 1, human | Orvepitant maleate | Hemokinin 1 (mouse) | Men 10376 TFA | Neurokinin A(4-10) TFA | NKP608 | Vapreotide 品牌介绍: MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供最新最全的高品质小分子活性化合物；10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；设有专业的实验中心和严格的质控、验证体系；提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；产品的生物活性多经各国客户实验验证；Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；与世界各大制药公司及知名科研机构建立了长期的合作。