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VU 0364770

源叶(MedMol) 99%
  • 英文名:
  • VU 0364770
  • 别名:
  • 2-Pyridinecarboxamide, N-(3-chlorophenyl)-
  • CAS号:
  • 61350-00-3
  • 分子式:
  • C12H9ClN2O
  • 分子量:
  • 232.67
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S80838-2mg 99% ¥224.00元 5 - - - EA 加入购物车
源叶(MedMol) S80838-5mg 99% ¥400.00元 6 - - - EA 加入购物车
源叶(MedMol) S80838-10mg 99% ¥544.00元 6 - - - EA 加入购物车
源叶(MedMol) S80838-25mg 99% ¥720.00元 6 - - - EA 加入购物车
源叶(MedMol) S80838-50mg 99% ¥960.00元 5 - - - EA 加入购物车
源叶(MedMol) S80838-100mg 99% ¥1480.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S80838-200mg 99% ¥2880.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: VU0364770 is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively
  • 靶点: Rat mGlu4:290 nM (EC50);Human mGlu4:1.1 μM (EC50);mGlu6:6.8 μM (EC50);mGlu5:17.9 μM (EC50);GluR
  • 体内研究:
    VU0364770 exhibits suitable pharmacokinetic properties for systemic dosing in animal models. After intravenous administration, VU0364770 is rapidly clears from the systemic circulation (165 ml/min/kg) and exhibits a volume of distribution of 2.92 L/kg. VU0364770 is a highly protein-bound ligand displaying free fractions of 2.7 and 1.8% in human and rat plasma, respectively. VU0364770 also shows an improved pharmacokinetic profile relative to previously reported mGlu4 PAMs with enhanced central penetration and a total brain-to-plasma ratio of more than 1 after systemic administration of a 10 mg/kg dose. VU0364770 produces a dose-dependent reversal of haloperidol-induced catalepsy. VU0364770 dose-dependently reverses haloperidol (0.75 mg/kg)-induced catalepsy in rats, significant at doses of 10 to 56.6 mg/kg, after subcutaneous dosing (F6,69=8.04; p<0.001)
  • 参考文献:
    1. Jones CK, et al. The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease. J Pharmacol Exp Ther.
  • 溶解性: DMSO  :  ≥  100  mg/mL  (429.79  mM)
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 4.298 ml 21.49 ml 42.979 ml
    5 mM 0.86 ml 4.298 ml 8.596 ml
    10 mM 0.43 ml 2.149 ml 4.298 ml
    50 mM 0.086 ml 0.43 ml 0.86 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)


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