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VU0364770  ≥98%

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包装规格：50mg 100mg 250mg in glass bottle
溶解性：溶于DMSO(≥100mg/mL）
产品描述：基本信息 产品编号：V10215 产品名称：VU0364770 CAS: 61350-00-3   储存条件 粉末 -20℃ 四年     分子式： C12H9ClN2O 溶于液体 -80℃ 六个月 分子量： 232.67 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 47mg/mL (202.0mM) Ethanol 47mg/mL (202.0mM) Water Insoluble 体内（现配现用）     ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 4.2979mL 21.4897mL 42.9793mL 5mM 0.8596mL 4.2979mL 8.5959mL 10mM 0.4298mL 2.1490mL 4.2979mL 50mM 0.0860mL 0.4298mL 0.8596mL   生物活性 产品描述 一种有效的选择性 mGlu4 正变构调节剂 (PAM)。 靶点/IC50 mGlu4  1.1μM(EC50)   体外研究 VU0364770 is a selective positive allosteric modulator of mGlu4 in recombinant systems.VU0364770 is a potent PAM of multiple signaling pathways that enhances the response of the rat and human mGlu4 receptors to the endogenous agonist glutamate.VU0364770 produces a concentration-dependent potentiation of the response to an EC20 concentration of glutamate with EC50 of 1.1±0.2μM and increases the maximal response to glutamate from 100 to 227±17%.Because of concerns that this chemical scaffold might possess activity at MAO,full IC50 determinations is performed for VU0364770 at the MAO-A and MAO-B isoforms;these studies result in Kis of 8.5 and 0.72μM for human MAO-A and human MAO-B,respectively.When tested at a 10μM concentration at each mGlu receptor,VU0364770 exhibits weak PAM activity (4.3-fold left shift of the glutamate CRC) at mGlu6 and antagonist activity (3.3-fold right shift of the glutamate CRC) at mGlu5 (compare to the 16.5-fold left shift of the glutamate concentration-response for mGlu4 at 10μM).When further evaluated in a full concentration-response curve format,VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9±5.5μM and PAM activity at mGlu6 with a potency of 6.8±1.7μM (compare with the potency of VU0364770 on the rat mGlu4 receptor of 290±80nM). 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 (165ml/min/kg) and exhibits a volume of distribution of 2.92L/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 10mg/kg dose.VU0364770 produces a dose-dependent reversal of haloperidol-induced catalepsy.VU0364770 dosedependently reverses haloperidol (0.75mg/kg)-induced catalepsy in rats,significant at doses of 10 to 56.6mg/kg,after subcutaneous dosing (F6,69=8.04;p<0.001).   推荐实验方法(仅供参考) 激酶实验： The effects of VU0364770 on rat mGlu1 and mGlu5 are assessed by using calcium mobilization and measuring the glutamate concentration-response relationship in the presence and absence of 10μM VU0364770.Using a double-addition protocol,VU0364770 is added to the cells,followed 2.5 min later by a full concentration-response of glutamate.Shifts of the concentration-response relationship are used to assess potential potentiator (left shift of more than 2-fold) or antagonist (right shift of more than 2-fold or depression of the maximum response by at least 75%) activity of VU0364770.Compounds are further assessed for mGlu5 antagonist activity by performing a full concentration-response curve,starting at 30μM and serially diluted it by using 1:3 dilutions,in the presence of an EC80 concentration of glutamate.   动物实验:   Rats Adult male Sprague-Dawley rats,weighing 250 to 300g,are used.Rat are examined for catalepsy 30 min after the administration of either VU0364770 (1-56.6mg/kg s.c.),VU0364772 (1-56.6mg/kg s.c.),A2A antagonist (56.6mg/kg p.o.),Preladenant (0.03-30mg/kg p.o.),or vehicle.In the interaction studies rats ate administered VU0364770 (10 or 30mg/kg)+vehicle,VU0364770 (10 or 30mg/kg)+Preladenant (0.1-1mg/kg), or vehicle+Preladenant (0.1-1mg/kg) 30 min before testing.
保存条件：-20℃

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