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. : 500-92-5
MCE 国际站:Proguanil
产品活性:Proguanil 是一种抗疟前体,被代谢为活性代谢物环鸟苷 (HY-12784)。Proguanil 是一种二氢叶酸还原酶 (DHFR) 抑制剂。
研究领域:Anti-infection | Cell Cycle/DNA Damage
作用靶点:Parasite | Antifolate
In Vitro: Proguanil per se has only weak antimalarial activity in vitro (IC50=2.4-19 μM), and its effectiveness depends on the active metabolite Cycloguanil (IC50=0.5-2.5 nM). The Cycloguanil is a dihydrofolate reductase (DHFR) inhibitor. The combination of Atovaquone and Proguanil is synergistic in vitro. Both drugs also have activity against gametocytes and pre-erythrocytic (hepatic) stages of malaria parasites.
Proguanil acts as a biguanide rather than as its metabolite Cycloguanil (a parasite dihydrofolate reductase [DHFR] inhibitor) to enhance the Atovaquone effect. Proguanil-mediated enhancement is specific for Atovaquone, since the effects of other mitochondrial electron transport inhibitors, such as Myxothiazole and Antimycin, are not altered by inclusion of Proguanil.
5-HT3 receptor responses are reversibly inhibited by Proguanil, the metabolite 4-chlorophenyl-1-biguanide (CPB) and the active metabolite Cycloguanil (CG), with an IC50 of 1.81, 1.48 and 4.36 μM, respectively.
In Vivo: Proguanil (p.o.; 2.9 mg/kg body weight; daily for 5 days and 6 weeks respectively) shows mild degenerative changes for five days, while shows severe degenerative changes for six weeks in wistar strain albino rats.
Serum testosterone level is significantly decreased for proguanil treatment rats.
Administration of Malarone (atovaquone and proguanil) to experimentally B. gibsoni infected two dogs in chronic stage and three dogs in acute stage results in decrease in parasitemia, and clinical improvements are observed.
相关产品:Drug Repurposing Compound Library Plus | FDA-Approved Drug Library Plus | FDA-Approved Drug Library Mini | Bioactive Compound Library Plus | Anti-Infection Compound Library | Cell Cycle/DNA Damage Compound Library | FDA-Approved Drug Library | Antiviral Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | Orally Active Compound Library | FDA Approved & Pharmacopeial Drug Library | Drug-Induced Liver Injury (DILI) Compound Library | Antiparasitic Compound library | Anti-Cancer Metabolism Compound Library | Children’s Drug Library | Human Metabolite Library | Off-patent Drug Library | Antifungal agent 26 | Quinidine-d3 | Angulatin G | Acridine Orange base | N-Desethyl amodiaquine-d5 | Palitantin | Proguanil-d6 | Azlocillin sodium salt | Methyl palmitate | HBPC–GSH | Doxycycline calcium | SQ109 | 13,21-Dihydroeurycomanone | Nevirapine | Monensin sodium salt | Clindamycin phosphate | 1-Deacetylnimbolinin B | KDU731 | (E)-Fenpyroximate | Niclosamide monohydrate | Antimalarial agent 8 | Geranin A | Cabamiquine | Harpagide | Clopidol | trans-Methylisoeugenol | Morantel tartrate | Berberine | Antileishmanial agent-17
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 | 抗体 | 点击化学
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
品牌介绍:
• MCE (MedChemExpress) 拥有200 多种全球独家化合物库,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;
• 50,000 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;
• 产品种类涵盖各种重组蛋白,多肽,常用试剂盒 ,更有 PROTAC、ADC 等特色产品,广泛应用于新药研发、生命科学等科研项目;
• 提供虚拟筛选,离子通道筛选,代谢组学分析检测分析,药物筛选等专业技术服务;
• 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。