Dimemorfan phosphate NEW
Price | $37 |
Package | 100mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-12 |
Product Details
Product Name: Dimemorfan phosphate | CAS No.: 36304-84-4 |
Purity: 99.67% | Supply Ability: 10g |
Release date: 2024/11/12 |
Product Introduction
Bioactivity
名稱 | Dimemorfan phosphate |
描述 | Dimemorfan phosphate (3,17-dimethylmorphinan) is a sigma 1 receptor agonist. Dimemorfan phosphate is used as a potent antitussive. |
體外活性 | Dimemorfan, at concentrations of 5-20 μM, concentration-dependently inhibits ROS production induced by fMLP and PMA, demonstrating greater potency against fMLP-induced ROS with an IC50 of 7.0 μM. At higher concentrations (10-50 μM), it does not significantly scavenge free radicals in the xanthine/xanthine oxidase system. Moreover, Dimemorfan effectively reduces Mac-1 upregulation and notably suppresses ROS and NO production induced by LPS in the 10-20 μM range. It also diminishes LPS-induced iNOS protein expression and decreases both the percentage and the median channel fluorescence (MCF) intensities of MCP-1 and TNF-α in the BV2 cytosol. At a concentration of 20 μM, Dimemorfan significantly inhibits the degradation of cytosolic Iκ-Bα, hinders the nuclear translocation of NF-κB p65, and curtails the transcriptional activity of NF-κB, showcasing its multifaceted inhibitory effects on inflammation-related mechanisms. |
體內(nèi)活性 | Dimemorfan, administered subcutaneously at doses of 6.25 or 12.5 mg/kg, significantly reduces BAY k-8644-induced convulsive behaviors in mice in a dose-dependent manner, as evidenced by a comparison of groups receiving dimemorfan and BAY k-8644 (6.25 mg/kg or 12.5 mg/kg) versus a control group treated with saline and BAY k-8644 (P<0.05 and P<0.01, respectively). Additionally, dimemorfan markedly decreases the BAY k-8644-stimulated elevation of c-fos and c-jun protein expression, also in a dose-related fashion. Notably, dimemorfan does not significantly impact mice's locomotor activity nor induce notable circling behavior. Moreover, intraperitoneal injections of dimemorfan (1 and 5 mg/kg) suppress the rise in plasma TNF-α levels in mice. Furthermore, dimemorfan treatment effectively hampers the infiltration of neutrophils into the lung and liver as well as decreases oxidative stress, evidenced by EB staining, in these organs following LPS challenge. |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | H2O : 10 mM DMSO : Insoluble |
關(guān)鍵字 | Dimemorfan Phosphate | inhibit | Inhibitor | Sigma Receptor | Dimemorfan phosphate | Dimemorfan |
相關(guān)產(chǎn)品 | KB-5492 free base | Cutamesine dihydrochloride | Blarcamesine hydrochloride | Amitriptyline hydrochloride | S1R agonist 2 | Ditolylguanidine | Sigma-1 receptor antagonist 1 | Glycerol phenylbutyrate | KSK67 | AB21 HCl |
相關(guān)庫 | 表型篩選靶點鑒定庫 | 經(jīng)典已知活性庫 | 膜蛋白靶向化合物庫 | 藥物功能重定位化合物庫 | NO PAINS 化合物庫 | 抗癌上市藥物庫 | 已知活性化合物庫 | GPCR靶點分子庫 | 抗癌化合物庫 | 抗癌藥物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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