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      114778-60-8
      • names:

        BRL44385

      • CAS號:

        114778-60-8

        MDL Number: MFCD00871933
      • MF(分子式): C8H11N5O3 MW(分子量): 225.2
      • EINECS: Reaxys Number:
      • Pubchem ID:135409371 Brand:BIOFOUNT
      BRL44385
      BRL44385(114778-60-8)有效且選擇性地抑制單純皰疹病毒1型和2型(HSV-1和HSV-2),水痘帶狀皰疹病毒(VZV)和Epstein-Barr病毒(EBV)復制。
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      中文別名 BRL44385(114778-60-8);9-(3-羥基丙氧基)鳥嘌呤;BRL 44385;BRL-44385;
      英文別名 BRL44385(114778-60-8);9-(3-hydroxypropoxy)guanine;BRL 44385;BRL-44385;
      CAS號 114778-60-8
      Inchi InChI = 1S / C8H11N5O3 / c9-8-11-6-5(7(15)12-8)10-4-13(6)16-3-1-2-14 / h4,14H,1-3H2, (H3,9,11,12,15)
      InchiKey UWCACOXRVYDNEE-UHFFFAOYSA-N
      分子式 Formula C8H11N5O3
      分子量 Molecular Weight 225.2
      溶解度Solubility
      性狀 Solid
      儲藏條件 Storage conditions 存放在陰涼干燥處

      BRL44385(114778-60-8)實驗注意事項:
      1.實驗前需戴好防護眼鏡,穿戴防護服和口罩,佩戴手套,避免與皮膚接觸。
      2.實驗過程中如遇到有毒或者刺激性物質及有害物質產生,必要時實驗操作需要手套箱內完成以免對實驗人員造成傷害
      3.實驗后產生的廢棄物需分類存儲,并交于專業生物廢氣物處理公司處理,以免造成環境污染Experimental considerations:
      1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
      2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

      Tags:BRL44385,BRL44385,BRL44385,BRL44385,BRL44385,BRL44385,BRL44385,BRL44385,BRL44385,BRL44385,
      產品說明 BRL44385(114778-60-8)是一種新型鳥嘌呤類似物,是1型和2型單純皰疹病毒和水痘帶狀皰疹病毒的有效和選擇性抑制劑。
      IntroductionBRL44385(114778-60-8)is a potent and selective inhibitor of the replication of herpes simplex virus types 1 and 2 (HSVandHSV2), varicella zoster virus (VZV) and Epsteinarr virus (EBV).
      Application1
      Application2
      Application3

      BRL44385(114778-60-8)藥理學:
      BRL44385是一種新型鳥嘌呤類似物,是1型和2型單純皰疹病毒和水痘帶狀皰疹病毒的有效和選擇性抑制劑。
      M. R. Harnden, et al. Synthesis, oral bioavailability and in vivo activity of acetal derivatives of the selective antiherpesvirus agent 9-(3-hydroxypropoxy) guanine (SRL 44385). Antiviral Chemistry &
      Use of rat and human in vitro systems to assess the effectiveness and enzymology of deoxyguanine analogs as prodrugs of an antiviral agent PMID 8013273; Drug metabolism and disposition: the biological
      Penciclovir is a selective inhibitor of hepatitis B virus replication in cultured human hepatoblastoma cells Antimicrobial agents and chemotherapy8723485 1996-05-01
      Synthesis and antiviral activity of 9-alkoxypurines. 1. 9-(3-Hydroxypropoxy)- and 9-[3-hydroxymethyl)propoxy]purines Journal of medicinal chemistry2153202 1990-01-01
       
      BRL44385(114778-60-8)參考文獻:
      1.Use of rat and human in vitro systems to assess the effectiveness and enzymology of deoxyguanine analogs as prodrugs of an antiviral agent.
      Harrell AW;Wheeler SM;East P;Clarke SE;Chenery RJ Drug Metab Dispos. 1994 Mar-Apr;22(2):189-93.

      BRL 55792, BRL 55791, and BRL 55039 are prodrugs of an active antiviral agent 9-(3-hydroxypropoxy) guanine (BRL 44385). The prodrugs were 6-deoxygenated analogs of BRL 44385, with ether groups substituted at the 9-position: BRL 55792 with an (isopropoxymethyloxy)propoxy group, BRL 55791 with a (methoxymethyloxy)propoxy group, and BRL 55039 with an ethoxypropoxy group. Conversion of the prodrugs to BRL 44385 had been demonstrated in vivo in the rat and involved 6-oxidation followed by dealkylation. Metabolism was studied in rat liver in vitro systems to find a model to evaluate BRL 44385 production. Rat hepatocytes performed both reaction steps and were used to assess which of the three prodrugs demonstrated greatest production of the active drug. BRL 55792 demonstrated greatest conversion in vitro, and this was in agreement with in vivo data. The production of BRL 44385 from BRL 55792 was also demonstrated in human hepatocyte incubations, providing evidence that these reactions can occur in humans, thereby increasing confidence that BRL 55792 would be suitable prodrug for human therapy. Further experiments were performed to investigate the enzymes involved in these conversions. The 6-oxidation step occurred in the cytosol.

      2.Use of rat and human in vitro systems to assess the effectiveness and enzymology of deoxy-guanine analogues as prodrugs of an antiviral agent.
      Harrell AW;Wheeler SM;East P;Clarke SE;Chenery RJ Drug Metab Dispos. 1994 Jan-Feb;22(1):124-8.

      BRL 55792, BRL 55791, and BRL 55039 are prodrugs of an active anti-viral agent 9-(3-hydroxypropoxy) guanine, (BRL 44385). The prodrugs were 6-deoxygenated analogues of BRL 44385 with ether groups substituted at the 9-position: BRL 55792 with an (isopropoxymethyloxy)propoxy group, BRL 55791 with a (methoxymethyloxy)propoxy group, and BRL 55039 with an ethoxypropoxy group. Conversion of the prodrugs to BRL 44385 had been demonstrated in vivo in rat and involved 6-oxidation followed by dealkylation. Metabolism was studied in rat liver in vitro systems to find a model to evaluate BRL 44385 production. Rat hepatocytes performed both reaction steps and were used to assess which of the three prodrugs demonstrated greatest production of the active drug. BRL 55792 demonstrated greatest conversion in vitro and this was in agreement with in vivo data. The production of BRL 44385 from BRL 55792 was also demonstrated in human hepatocyte incubations providing evidence that these reactions can occur in man thereby increasing confidence that BRL 55792 would be a suitable prodrug for human therapy. Further experiments were performed to investigate the enzymes involved in these conversions. The 6-oxidation step occurred in the cytosol.

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