CAS: 599179-03-0; (4,6-Dimethylpyrimidin-5-yl)(4-((S)-4-((R)-2-Methoxy-1-(4-(Trifluoromethyl)Phenyl)Ethyl)-3-Methylpiperazin-1-yl)-4-Methylpiperidin-1-yl)Methanone Maleate
该化合物是CCR5化学受体的小型分子对立体,在艾滋病毒-1病毒进入宿主细胞方面起着关键作用.作为一种雄性盐配方,它表现出了比其免费基底配方更好的溶性性和生物利用率.该化合物表明CCR5对其他化学受体具有高度选择性,最大限度地减少离目标效果.其行动机制涉及对CCCR5受体的过敏抑制,有效阻塞 gp120 介质聚变过程.在临床研究中,Vicrivironoc 雄性在R5-troHIV-1菌株方面表现出强大的抗病毒活动,在混合疗法中使用时具有有利的抗药性特征.性盐形式加强了化合物的物理化学特性,有助于更加一致的药用皮肤化学性能.其分子结构允许渗透到包括...
- 英文名称(4,6-Dimethylpyrimidin-5-yl)(4-((S)-4-((R)-2-Methoxy-1-(4-(Trifluoromethyl)Phenyl)Ethyl)-3-Methylpiperazin-1-yl)-4-Methylpiperidin-1-yl)Methanone Maleate
- 中文名称1-[(4,6-二甲基-5-嘧啶基)羰基]-4-[(3S)-4-[(1R)-2-甲氧基-1-[4-(三氟甲基)苯基]乙基]-3-甲基-1-哌嗪基]-4-甲基哌啶马来酸盐
- IUPAC名称Vicriviroc maleate
- 其它别名Vicriviroc Maleate [mi]; (Z)-But-2-Enedioic Acid; (4,6-Dimethylpyrimidin-5-yl)-[4-[(3S)-4-[(1R)-2-Methoxy-1-[4-(Trifluoromethyl)Phenyl]Ethyl]-3-Methylpiperazin-1-Yl]-4-Methylpiperidin-1-Yl]Methanone; Vicriviro
- CAS编号599179-03-0
- MFCD编号:MFCD09833218
- EINECS号:682-748-3
- FDA UNII编号:EP3QG127N9
- 分子式:C32H42F3N5O6分子量:649.71
- 产品CID: 1576104
- 同类组份化合物CAS306296-47-9 (free base)541503-81-5 (malate)599179-03-0 (maleate)541503-48-4 (HCl)
- 产品分类生物化工 → 生化试剂 → 激动剂抑制剂
物理性质
- 沸点608.1 °C at 760mmHg
- 闪点608.1°Cat760mmHg
- PSA:136.4
- LogP:4.0262
- 溶解性DMSO: 50 mg/mL (76.96 Mm; Need Ultrasonic)H2O: 25 mg/mL (38.48 Mm; Need Ultrasonic And Warming)
- 外观形态白色至类白色粉末
- 储存条件储存在 -20°C
- 产品应用该化合物用作阻止艾滋病毒-1进入和复制周边的单一血液细胞(PBMCS);它表明对一大批艾滋病毒-1隔离物,包括小FL,ADA-M,301657,301657,JV1083和RU570等临床菌株的抗病毒活动;它还抑制CCCRC5对MIP-1Α的化学反应,并抑制RANTES诱发的信号,表明其在治疗CRR5-热带艾滋病毒-1感染方面的潜在应用.
MSDS等安全信息
欧盟法规
C&L通报合成工艺路线路线简述
海关参考信息
- 2901210000-乙烯
2901220000-丙烯
2902600000-乙苯
2912110000-甲醛 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
供应商参考报价(招募中)
品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1: Liu AY, Zhang J, Anderson PL, Wagner T, Pan Z, Peda M, Gomez K, Beamer M, Jacobson C, Strizki J, Dezzutti CS, Piper JM; MTN-028 Protocol Team for the Microbicide Trials Network. Phase 1 Pharmacokinetic Trial of 2 Intravaginal Rings Containing Different Dose Strengths of Vicriviroc (MK-4176) and MK-2048. Clin Infect Dis. 2019 Mar 19;68(7):1129-1135. doi: 10.1093/cid/ciy652.
2: Hoesley CJ, Chen BA, Anderson PL, Dezzutti CS, Strizki J, Sprinkle C, Heard F, Bauermeister J, Hall W, Jacobson C, Berthiaume J, Mayo A, Gundacker H, Richardson-Harman N, Piper J; Microbicide Trials Network 027 Study Team. Phase 1 Safety and Pharmacokinetics Study of MK-2048/Vicriviroc (MK-4176)/MK-2048A Intravaginal Rings. Clin Infect Dis. 2019 Mar 19;68(7):1136-1143. doi: 10.1093/cid/ciy653.
3: Hesk D, Borges S, Hendershot S, Koharski D, McNamara P, Ren S, Saluja S, Truong V, Voronin K. Synthesis of (3) H, (2) H4 and (14) C-SCH 417690 (Vicriviroc). J Labelled Comp Radiopharm. 2016 May 15;59(5):190-6. doi: 10.1002/jlcr.3387. Epub 2016 Mar 14. 10(1):15. doi: 10.1186/1742-6405-10-15.
合成参考文献
参考文献:10.1128/aac.49.12.4911-4919.2005
摘要:Strizki JM, Tremblay C, Xu S, Wojcik L, Wagner N, Gonsiorek W, Hipkin RW, Chou C, Pugliese-Sivo C, Xiao Y, Tagat JR, Cox K, Priestley T, Sorota S, Huang W, Hirsch M, Reyes GR, Baroudy BM. Discovery and Characterization of Vicriviroc (SCH 417690), a CCR5 Antagonist with Potent Activity against Human Immunodeficiency Virus Type 1. Antimicrob Agents Chemother. 2005 Dec;49(12):4911–9. doi: 10.1128/aac.49.12.4911-4919.2005.
📝 需求与反馈
尽可能描述清楚需求与问题信息
