JZL-195抑制剂 | 1210004-12-8

• 物质功能分类: 生物化工 - 生化试剂 - 激动剂抑制剂
• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: JZL-195抑制剂
• 中文别名: 4-[（3-苯氧基苯基）甲基]-1-哌嗪羧酸4-硝基苯酯盐酸盐，
• 英文名称: (4-Nitrophenyl) 4-[(3-phenoxyphenyl)methyl]piperazine-1-carboxylate
• CAS: 1210004-12-8
• 化学式: C24H23N3O5
• 分子量: 433.5
• InChiKey: QNYRAEKLMNDRFY-UHFFFAOYSA-N

物化性质

• 沸点：
  581.8±50.0 °C(Predicted)
• 密度：
  1.303±0.06 g/cm3(Predicted)
• 溶解度：
  加热时在DMSO中的溶解度≥5mg/mL

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  32
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  87.8
• 氢给体数：
  0
• 氢受体数：
  6

制备方法与用途

生物活性

JZL195是有效的FAAH和MAGL抑制剂，IC50分别为2 nM和4 nM。

靶点

Target	Value
FAAH ()	2 nM
MAGL ()	4 nM

体外研究

JZL195 produces near-complete blockade of FP-Rh labeling of both mouse brain FAAH and MAGL at concentrations as low as 100 nM (IC ₅₀ values of 13 and 19 nM, respectively).
JZL195 inhibits rat and human FAAH and MAGL enzymes with IC ₅₀ values in the range of ≈10-100 nM based on competitive ABPP assays.

体内研究

JZL195 (20 mg/kg; i.p.) produces an antinociceptive response in the tail immersion assay.

Animal Model:	Male C57BL/6J mice
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection
Result:	Produced a much greater antinociceptive response in the tail immersion assay compared with inhibitors of either FAAH or MAGL alone.

文献信息

• CHROMENIC PHYTOCANNABINOIDS, THEIR SYNTHESIS AND USE IN TREATMENT OR PREVENTION OF DISEASE
  申请人：Emerald Health Biotechnology España,S.L.U.

  公开号：EP3666765A1

  公开（公告）日：2020-06-17

  The present invention relates to a compound of the formula (I) or a solvate or co-crystal thereof wherein: - R is selected from the group consisting of: a C1-C6 alkyl, a C2-C8 alkenyl moiety, a C4-C12 dienyl or a C6-C18 trienyl moiety; - R1 is a C1-C6 alkyl moiety; - R2 is selected from the group consisting of: H and a C1-C6 alkyl moiety; - R3 is selected from the group consisting of: H and a C1-C6 alkyl moiety; - R4 is selected from the group consisting of: H, a C1-C6 alkyl moiety and a benzyl moiety. The present invention also relates to a process for producing said compound of the formula (I), or a solvate or co-crystal thereof, as well as a pharmaceutical composition comprising said compound of the formula (I), or a solvate or co-crystal thereof and at least one excipient. The present invention also relates to a compound of the formula (I), or a solvate or co-crystal thereof, for use in the treatment or prevention of a disease or condition.

  本发明涉及以下公式(I)的化合物或其溶剂或共晶体，其中：- R选自以下组：C1-C6烷基，C2-C8烯基基团，C4-C12二烯基或C6-C18三烯基；- R1是C1-C6烷基基团；- R2选自以下组：H和C1-C6烷基基团；- R3选自以下组：H和C1-C6烷基基团；- R4选自以下组：H，C1-C6烷基基团和苄基。本发明还涉及制备所述公式(I)的化合物或其溶剂或共晶体的方法，以及包括所述公式(I)的化合物或其溶剂或共晶体和至少一种赋形剂的药物组合物。本发明还涉及用于治疗或预防疾病或状况的公式(I)的化合物或其溶剂或共晶体。
• METHODS OF TREATING RENAL DISEASE
  申请人：The Regents of the University of California

  公开号：EP3823610A1

  公开（公告）日：2021-05-26
• [EN] A GPR119-BASED SIGNALING SYSTEM IN THE MURINE EYE REGULATES INTRAOCULAR PRESSURE IN A SEX-DEPENDENT MANNER<br/>[FR] SYSTÈME DE SIGNALISATION À BASE DE GPR119 DANS L'ŒIL MURIN RÉGULANT LA PRESSION INTRAOCULAIRE EN FONCTION DU SEXE
  申请人：UNIV INDIANA RES & TECH CORP

  公开号：WO2017222713A1

  公开（公告）日：2017-12-28

  Methods of activating a GPR119-based signaling system in the mammalian eye are disclosed. More particularly, activation of the GPR119-based signaling system has been found to reduce intraocular pressure (IOP) in female mammalian eyes, providing a potential treatment for glaucoma.
• [EN] METHODS OF TREATING RENAL DISEASE<br/>[FR] MÉTHODES DE TRAITEMENT D'UNE MALADIE RÉNALE
  申请人：UNIV CALIFORNIA

  公开号：WO2020018554A1

  公开（公告）日：2020-01-23

  Disclosed herein, inter alia, are methods of treating renal disease (e.g., chronic kidney disease or end stage renal disease).
• [EN] CHROMENIC PHYTOCANNABINOIDS, THEIR SYNTHESIS AND USE IN TREATMENT OR PREVENTION OF DISEASE<br/>[FR] PHYTOCANNABINOÏDES CHROMÉNIQUES, LEUR SYNTHÈSE ET LEUR UTILISATION DANS LE TRAITEMENT OU LA PRÉVENTION D'UNE MALADIE
  申请人：EMERALD HEALTH BIOTECHNOLOGY ESPANA S L U

  公开号：WO2020120582A1

  公开（公告）日：2020-06-18

  The present invention relates to a compound of the formula (I) or a solvate or co-crystal thereof (I) wherein: - R is selected from the group consisting of: a C1-C6 alkyl, a C2-C8 alkenyl moiety, a C4-C12 dienyl or a C6-C18 trienyl moiety; - R1 is a C1-C6 alkyl moiety; - R2 is selected from the group consisting of: H and a C1-C6 alkyl moiety; - R3 is selected from the group consisting of: H and a C1-C6 alkyl moiety; - R4 is selected from the group consisting of: H, a C1-C6 alkyl moiety and a benzyl moiety. The present invention also relates to a process for producing said compound of the formula (I), or a solvate or co-crystal thereof, as well as a pharmaceutical composition comprising said compound of the formula (I), or a solvate or co-crystal thereof and at least one excipient. The present invention also relates to a compound of the formula (I), or a solvate or co-crystal thereof, for use in the treatment or prevention of a disease or condition.