JNJ-1661010

• 常用名: JNJ-1661010
• 英文名: JNJ-1661010
• CAS号: 681136-29-8
• 分子量: 365.452
• 密度: 1.3±0.1 g/cm3
• 沸点: N/A
• 分子式: C₁₉H₁₉N₅OS
• 熔点: 240.48 °C
• 闪点: N/A

JNJ-1661010用途

JNJ-1661010 (Takeda-25) 是一种有效的选择性脂肪酸酰胺水解酶 (FAAH) 抑制剂,对大鼠和人FAAH 的 IC50 分别为 34 和 33 nM。JNJ-1661010 可以穿透血脑屏障,用作广谱镇痛药。

JNJ-1661010名称

• 英文名: N-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide

JNJ-1661010生物活性

• 描述: JNJ-1661010 (Takeda-25) 是一种有效的选择性脂肪酸酰胺水解酶 (FAAH) 抑制剂,对大鼠和人FAAH 的 IC50 分别为 34 和 33 nM。JNJ-1661010 可以穿透血脑屏障,用作广谱镇痛药。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> FAAH
  研究领域 >> 神经疾病
  信号通路 >> 神经信号通路 >> FAAH
• 靶点实验:

  IC50: 34 nM (rat FAAH) and 33 nM (human FAAH)[1]

• 体内研究: JNJ-1661010(武田-25；i.p.；50mg/kg)减轻炎症大鼠角叉菜胶爪子模型的热痛觉过敏[2]。JNJ-1661010(i.p.；10 mg/kg)对大鼠的T1/2为35分钟,CL为0.032 mL/min/kg,Cmax为1.58μM[1]。
• 参考文献:

  [1]. Keith JM, et al. Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4838-43.

  [2]. Karbarz MJ, et al. Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylicacid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase. Anesth Analg. 2009 Jan;108(1):316-29.

JNJ-1661010物理化学性质

• 密度: 1.3±0.1 g/cm3
• 熔点: 240.48 °C
• 分子式: C₁₉H₁₉N₅OS
• 分子量: 365.452
• 精确质量: 365.131042
• PSA: 89.60000
• LogP: 2.57
• InChIKey: BHBOSTKQCZEAJM-UHFFFAOYSA-N
• SMILES: O=C(Nc1ccccc1)N1CCN(c2nc(-c3ccccc3)ns2)CC1
• 外观性状: 固体
• 折射率: 1.679
• 储存条件: Store at +4°C
• 水溶解性: DMSO: ≥28mg/mL

JNJ-1661010靶点实验

查看更多实验

实验名称：Primary cell-based high-throughput screening assay for identification of compounds th... 来源：Johns Hopkins Ion Channel Center 靶标：regulator of G-protein signaling 4 isoform 2 [Homo sapiens] External Id：JHICC_RGS_Act_HTS

实验名称：Luminescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：mu-type opioid receptor isoform MOR-1 [Homo sapiens] External Id：OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN

实验名称：Apparent inhibition of human FAAH expressed in CHO-K1 cells using ethanolamine 1-3[H]... 来源：ChEMBL 靶标：Fatty-acid amide hydrolase 1 External Id：CHEMBL2327495

实验名称：Primary qHTS assay for small molecule inhibitors of Inositol hexaphosphate kinase 1 (... 来源：NCGC External Id：IP6K1-p1

实验名称：QFRET-based biochemical primary high throughput screening assay to identify exosite i... 来源：The Scripps Research Institute Molecular Screening Center 靶标：disintegrin and metalloproteinase domain-containing protein 17 preproprotein [Homo sapiens] External Id：ADAM17_INH_QFRET_1536_1X%INH PRUN

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：Human Fatty acid amide hydrolase (Hydrolases) 来源：IUPHAR-DB 靶标：Fatty acid amide hydrolase (Hydrolases) [Homo sapiens] External Id：1400_Human

实验名称：Cytochrome P450 family 3 subfamily A member 4 (CYP3A4) small molecule antagonists: lu... 来源：NCGC External Id：CYP3A4437

实验名称：Cytochrome P450 family 2 subfamily D member 6 (CYP2D6) small molecule antagonists: lu... 来源：NCGC External Id：CYP2D6395

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JNJ-1661010英文别名

• N1-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide
• N-Phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide
• N-Phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)-1-piperazinecarboxamide