CAS: 273404-37-8; (S)-1-((S)-2-(4-Amino-3-Chlorobenzamido)-3,3-Dimethylbutanoyl)-N-((2R,3S)-2-Ethoxy-5-Oxotetrahydrofuran-3-yl)Pyrrolidine-2-Carboxamide
该化合物是VRT-043198的抗药剂,一种强效(KI=0.8 nM ICE/caspasase-1; <0.6nM caspase-4)和选择性抑制剂,它有选择地抑制了内 Leukin对酶/cstas-1子家族的胃胃炎,1 VRT-043198 IC/Caspase-1 IC50 = 0.67 M PBMCs,1.0 M 整血,它阻止人体体外单细胞释放IL-1b和IL-18,并阻止其在发炎模型中活性生产. Belnacasan抑制了NLRP3的活化和表达,导致慢性轻度应激2 引发的抑制性类似抑制性行为的温和性2 和防止多发性硬质病模型中的液性淋病.
- 英文名称(S)-1-((S)-2-(4-Amino-3-Chlorobenzamido)-3,3-Dimethylbutanoyl)-N-((2R,3S)-2-Ethoxy-5-Oxotetrahydrofuran-3-yl)Pyrrolidine-2-Carboxamide
- 中文名称N-(4-氨基-3-氯苯甲酰基)-3-甲基-L-缬氨酰-N-[(2R,3S)-2-乙氧基四氢-5-氧代-3-呋喃基]-L-脯氨酰胺
- IUPAC名称(S)-1-((S)-2-(4-amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)-N-((2R,3S)-2-ethoxy-5-oxotetrahydrofuran-3-yl)pyrrolidine-2-carboxamide
- 其它别名1-((2S)-2-((4-Amino-3-Chlorobenzoyl)Amino)-3,3-Dimethylbutanoyl)-N-((2R,3S)-2- Ethoxy-5-Oxo-Tetrahydrofuran-3-yl)-L-Prolinamide; Belnacasan [usan:Inn]; N-(4-Amino-3-Chloroben
- CAS编号273404-37-8
- MFCD编号:MFCD23102811
- EINECS号:695-154-4
- FDA UNII编号:00OLE78529
- 分子式:C24H33ClN4O6分子量:509.0
- 产品CID: 1253494
- 产品分类生物化工 → 抑制剂 → 细胞凋亡(Apoptosis)
物理性质
上下游产品
4-amino-3-chlorobenzoic acid (S)-N-carbobenzoxy-tert-butylleucine 1-[2-(4-amino-3-chlorobenzoylamino)-3,3-dimethylbutyryl]pyrrolidine-2-carboxylic acid tert-butyl ester合成工艺路线路线简述
📜3-氯-4-氨基苯甲酸置于盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,N,N-二异丙基乙胺,三氟乙酸体系中,用 二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 39.84H,反应生成N-(4-氨基-3-氯苯甲酰基)-3-甲基-L-缬氨酰-N-[(2R,3S)-2-乙氧基四氢-5-氧代-3-呋喃基]-L-脯氨酰胺
参考文献:Prodrug Of An Ice Inhibitor
标题:Prodrug Of An Ice Inhibitor
摘要:该发明描述了一种具有非常好生物利用度的ice抑制剂前药(i).化合物i对于治疗il-1介导的疾病如类风湿性关节炎,炎症性肠病,克罗恩病,溃疡性结肠炎,炎性腹膜炎,脓毒性休克,胰腺炎,创伤性脑损伤,器官移植排斥反应,骨关节炎,哮喘,牛皮癣,阿尔茨海默病,心肌梗死,充血性心力衰竭,亨廷顿病,动脉粥样硬化,特应性皮炎,白血病及相关疾病,骨髓增生异常综合症,葡萄膜炎或多发性骨髓瘤具有用处.
海关参考信息
- 2903919090-氯苯
2905121000-正丙醇
2905130000-正丁醇
2905399002-1,4-丁二醇 - 💡 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: Zahid A, Li B, Kombe AJK, Jin T, Tao J. Pharmacological Inhibitors of the NLRP3 Inflammasome. Front Immunol. 2019 Oct 25;10:2538. doi: 10.3389/fimmu.2019.02538.
2: Tezcan G, Garanina EE, Alsaadi M, Gilazieva ZE, Martinova EV, Markelova MI, Arkhipova SS, Hamza S, McIntyre A, Rizvanov AA, Khaiboullina SF. Therapeutic Potential of Pharmacological Targeting NLRP3 Inflammasome Complex in Cancer. Front Immunol. 2021 Feb 3;11:607881. doi: 10.3389/fimmu.2020.607881.
3: Li ZJ, Dai HQ, Huang XW, Feng J, Deng JH, Wang ZX, Yang XM, Liu YJ, Wu Y, Chen PH, Shi H, Wang JG, Zhou J, Lu GD. Artesunate synergizes with sorafenib to induce ferroptosis in hepatocellular carcinoma. Acta Pharmacol Sin. 2021 Feb;42(2):301-310. doi: 10.1038/s41401-020-0478-3. Epub 2020 Jul 22.
合成参考文献
参考文献:10.1186/s13045-019-0755-0
摘要:Xu S, Li X, Liu Y, Xia Y, Chang R, Zhang C. Inflammasome inhibitors: promising therapeutic approaches against cancer. Journal of Hematology & Oncology. 2019 Jun 26;12(1):64. doi: 10.1186/s13045-019-0755-0.
参考文献:10.1038/s41582-019-0217-x
摘要:Vezzani A, Balosso S, Ravizza T. Neuroinflammatory pathways as treatment targets and biomarkers in epilepsy. Nat Rev Neurol. 2019 Aug;15(8):459–72. doi: 10.1038/s41582-019-0217-x.
参考文献:10.1038/s41419-020-02865-4
摘要:Johnson DC, Okondo MC, Orth EL, Rao SD, Huang H, Ball DP, Bachovchin DA. DPP8/9 inhibitors activate the CARD8 inflammasome in resting lymphocytes. Cell Death & Disease. 2020 Aug 14;11(8):628. doi: 10.1038/s41419-020-02865-4.
参考文献:10.1007/s11010-021-04293-0
摘要:Li M, Du X, Yuan Z, Cheng M, Dong P, Bai Y. Lentinan triggers oxidative stress-mediated anti-inflammatory responses in lung cancer cells. Molecular and Cellular Biochemistry. 2021 Nov 16;477(2):469–77. doi: 10.1007/s11010-021-04293-0.
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