MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。
CAS No. : 142569-99-1
MCE 国际站:IRL-1620
产品活性:IRL-1620 是高效,选择性的内啡肽受体 (endothelin receptor) B 型激动剂,Ki 值为 16 pM。
研究领域:GPCR/G Protein
作用靶点:Endothelin Receptor
In Vitro: IRL-1620 is the most potent and specific ligand for the ETB receptor (KiETA/ KiETB=120,000) as judged by the Ki values for ETA (19 μM) and ETB (16 PM) receptors. IRL-1620 is 60 times more selective for the ETB receptor than ET-3 (KiETA/ KiETB=1,900).
In Vivo: IRL-1620 (1-100 nM) induces contractions of the guinea pig trachea. The effective concentration that produces 30 % of 60 mM KCI-induced contraction is estimated to be 28 nM for IRL 1620. IRL-1620 (1-100 nM) increases cytosolic Ca2+ in the vascular endothelium ([Ca]E) with little effect on resting muscle tone, and relaxes the norepinephrine-stimulated tone with an increase in [Ca]E, in rat aorta,. IRL-1620 improves both acquisition (learning) and retention (memory) on the water maze task and enhances angiogenic and neurogenic remodeling. Rats treated with IRL-1620 significantly reduces the cognitive impairment induced by Aβ. IRL-1620 treatment enhances the number of blood vessels labeled with VEGF compared to vehicle treatment.IRL-1620, restores analgesic tolerance to morphine and oxycodone, but it does not affect morphine and oxycodone induced decrease in NGF/PI3K expression. IRL-1620 attenuates opioid tolerance without the involvement of NGF/PI3K pathway.
相关产品:BQ-788 | [Asn18] Endothelin-1, human | TBC3711 | BQ-3020 TFA | Sparsentan | [Lys4] Sarafotoxin S6c | Nebentan potassium | Bosentan | Endothelin 1 (swine, human) (TFA) | Ambrisentan | Ro 46-2005 | [Ala2] Endothelin-3, human | ZD-1611 | PD-159020 | Aminaftone | A-192621 | Macitentan | Sulfisoxazole | Endothelin-3, human, mouse, rabbit, rat TFA | IRL 2500 | Carperitide acetate | Atrial Natriuretic Peptide (ANP) (1-28), rat TFA | ACT-373898 | Kendomycin | Zibotentan | BQ-123 TFA
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
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前沿最全的高品质小分子活性化合物;
• 40,000 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TOP期刊及制药专利收录了MCE客户的科研成果;
• 专业团队跟踪前沿的制药及生命科学研究进展,为您提供全球前沿的活性化合物;
• 与世界各大制药公司及知名科研机构建立了长期的合作。