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JNJ-42153605

CAS No. 1254977-87-1

JNJ-42153605 ( JNJ-42153605 | JNJ 42153605 | JNJ42153605 )

产品货号. M17222 CAS No. 1254977-87-1

JNJ-42153605 是一种 mGlu2 受体正变构调节剂 (EC50: 17 nM)。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
2MG ¥664 有现货
5MG ¥1191 有现货
10MG ¥1750 有现货
25MG ¥3175 有现货
50MG ¥4771 有现货
100MG ¥6828 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    JNJ-42153605
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    JNJ-42153605 是一种 mGlu2 受体正变构调节剂 (EC50: 17 nM)。
  • 产品描述
    JNJ-42153605 is a potent and selective mGlu2 receptor PAM with an acceptable pharmacokinetic profile in rodent and nonrodent species. JNJ-42153605 showed centrally mediated in vivo effectivity in models sensitive to mGlu2 receptor modulation such as sleep?wake electroencephalogram (sw-EEG) in rats,34 showing suppressed REM sleep during the first 4 h after oral administration of a 3 mg/kg dose.
  • 体外实验
    JNJ-42153605 is assessed for its selectivity for the mGlu2 receptor and is found to not have agonist or antagonist activity toward other mGlu receptor subtypes up to 30 μM. JNJ-42153605 shows high permeability with no indication for P-glycoprotein efflux.
  • 体内实验
    JNJ-42153605 shows a central in vivo efficacy by inhibition of REM sleep state at a dose of 3 mg/kg po in the rat sleep-wake EEG paradigm, a phenomenon shown to be mGlu2 mediated. In mice, JNJ-42153605 shows reversed PCP-induced hyperlocomotion with an ED50 of 5.4 mg/kg sc, indicative of antipsychotic activity. JNJ-42153605 shows a rapid rate of absorption from the gastrointestinal tract, reaching the maximal concentration after 0.5 h. Clearance in vivo is moderate to high in both rat and dog (35 and 29 mL/min/kg, respectively). Elimination halflives are on the shorter side across the species, being 2.7 h in rat and 0.8-1.1 h in dog.
  • 同义词
    JNJ-42153605 | JNJ 42153605 | JNJ42153605
  • 通路
    Chromatin/Epigenetic
  • 靶点
    COX
  • 受体
    mGluR2 PAM
  • 研究领域
    ——
  • 适应症
    ——

化学信息

  • CAS Number
    1254977-87-1
  • 分子量
    400.45
  • 分子式
    C22H23F3N4
  • 纯度
    >98% (HPLC)
  • 溶解度
    In Vitro:?DMSO : 16.67 mg/mL (41.63 mM)
  • SMILES
    c12c(c(ccn1c(nn2)CC1CC1)N1CCC(CC1)c1ccccc1)C(F)(F)F
  • 化学全称
    3-(Cyclopropylmethyl)-7-(4-phenyl-1-piperidinyl)-8-(trifluoromethyl)[1,2,4]triazolo[4,3-a]pyridine

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1.Cid JM, et al. J Med Chem. 2012 Oct 25;55(20):8770-89.
产品手册
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