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。

MK-571 sodium

CAS No. : 115103-85-0

MCE 站：MK-571 sodium

产品活性：MK-571 (L-660711) sodium 是一种选择性，口服活性的白三烯D4受体拮抗剂，在豚鼠和人肺膜的K_i分别为0.22 和 2.1 nM。

研究领域：GPCR/G Protein

作用靶点：Leukotriene Receptor

In Vitro: MK-571 sodium is a potent ａnd selective competitive inhibitor of [³H]leukotriene D4 binding in guinea pig (K_i value, 0.22 nM) ａnd human (K_i value, 2.1 nM) lung membranes. MK-571 sodium is essentially inactive versus [³H]LTC4 binding with IC₅₀ values of 23±11 μM (n=16) ａnd 32 μM (n=1) in guinea pig ａnd human lung, respectively. MK-571 sodium competitively antagonizes contractions of guinea pig trachea ａnd ileum induced by leukotriene (LT) D₄ (respective pA₂ values, 9.4 ａnd 10.5) ａnd LTE4 (respective pA₂ values, 9.1 ａnd 10.4) ａnd contractions of human trachea induced by LTD₄ (pA₂ value, 8.5). MK-571 (58 nM) sodium antagonizes contractions of guinea pig trachea induced by LTC₄ in the absence (dose ratio=28) but not in the presence of 45 mM L-serine borate (dose ratio less than 2). MK-571 (19μM) sodium does not block contractions of guinea pig trachea induced by histamine, acetylcholine, 5-hydroxytryptamine, PGF₂ alpha, U-44069, or PGD₂. In the presence of atropine, mepyramine, ａnd indomethacin, MK-571 (19 μM) sodium inhibits a small component of the response to antigen on guinea pig trachea but completely blocked anti-IgE-induced contractions of human trachea.

In Vivo: MK-571 (L-660,711; i.v.) sodium antagonizes bronchoconstriction induced in anesthetized guinea pigs by i.v. LTC₄, LTD₄, ａnd LTE₄ but does not block bronchoconstriction to arachidonic acid, U-44069, 5-hydroxytryptamine, histamine, or acetylcholine. Intraduodenal MK-571 sodium antagonizes LTD₄ (0.2-12.8 μg/kg)-induced bronchoconstriction in guinea pigs, ａnd p.o. MK-571 sodium blockes LTD₄- ａnd Ascaris-induced bronchoconstriction in conscious squirrel monkeys ａnd ovalbumin-induced bronchoconstriction in conscious sensitized rats treated with methysergide (3 μg/kg). Hypoxia-exposed WT mice are treated with either saline or MK-571 (5 mg/kg/d or 25 mg/kg/d) sodium for 2 more weeks while being maintain in hypoxic conditions. Saline-treated mice display all the hallmarks of PH (i.e., an increase in RVSP, Fulton index, ａnd arterial wall thickness). However, following hypoxia, MK-571 sodium-treated mice display lower RVSP ａnd Fulton index ａnd a decrease in the medial thickening of small pulmonary arteries ａnd arterioles.

相关产品：Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Immunology/Inflammation Compound Library  |  Orally Active Compound Library  |  Montelukast sodium  |  MK-886  |  Zafirlukast  |  Pranlukast  |  Gemilukast  |  Fiboflapon  |  Leukotriene B4  |  Etalocib  |  LY255283  |  Nedocromil  |  CP-105696  |  (Rac)-HAMI 3379  |  5-O-Demethylnobiletin  |  BIIL-260 hydrochloride  |  LY223982  |  Darbufelone mesylate  |  (S)-Verapamil hydrochloride  |  11-Keto-beta-boswellic acid  |  RG-12525  |  Veliflapon  |  12S-HHT  |  AS-35  |  KP496  |  Quinotolast sodium  |  Tipelukast

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  染料试剂  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds

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*新*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 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*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。