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VU 0364770

VU 0364770 更多供应商
公司名称: 上海波以尔化工有限公司  
联系电话:
产品介绍: 英文名称:VU 0364770
CAS:61350-00-3
公司名称: 北京百灵威科技有限公司  
联系电话: 010-82848833 400-666-7788
产品介绍: 英文名称:N-(3-Chlorophenyl)-2-pyridinecarboxaMide
CAS:61350-00-3
包装信息:100Mg,10Mg 备注:化学试剂、精细化学品、医药中间体、材料中间体
公司名称: 北京华威锐科化工有限公司  
联系电话: 0757-86329057 18516978288
产品介绍: 英文名称:N-(3-chlorophenyl)pyridine-2-carboxamide
CAS:61350-00-3
纯度:98.00% 包装信息:1g
公司名称: 南京康满林化工实业有限公司  
联系电话: 025-83697070
产品介绍: 英文名称:2-PyridinecarboxaMide, N-(3-chlorophenyl)-
CAS:61350-00-3
纯度:97%. 包装信息:5g;1kg;10kg 备注:1g-25g小包装请到商城订购;大量及定制请联系客服报价
公司名称: BOC Sciences  
联系电话: 16314854226
产品介绍: 英文名称:VU 0364770
CAS:61350-00-3
最新发布供应信息
VU0364770_Shenzhen Tuoda Pharmatech Co., Ltd
2021/7/9 12:56:26
VU 0364770
生物活性靶点体外研究体内研究 MSDS 用途与合成方法 VU 0364770价格(试剂级) 上下游产品信息
中文名称:VU 0364770
中文同义词:N-(3-氯苯基)-2-吡啶甲酰胺;N-(3-氯苯基)吡啶甲酰胺
英文名称:VU 0364770
英文同义词:VU 0364770;2-PyridinecarboxaMide, N-(3-chlorophenyl)-;N-(3-Chlorophenyl)picolinamide;N-(3-chlorophenyl)pyridine-2-carboxamide;VU 0364770 100MG;VU0364770;VU-0364770;VU 0364770 USP/EP/BP;SKL856
CAS号:61350-00-3
分子式:C12H9ClN2O
分子量:232.67
EINECS号:
相关类别:小分子抑制剂,天然产物;神经信号;Aromatics, Heterocycles;Inhibitors
Mol文件:61350-00-3.mol
VU 0364770
VU 0364770 性质
熔点 81-83 °C
沸点 293.6±20.0 °C(Predicted)
密度 1.341±0.06 g/cm3(Predicted)
储存条件 Inert atmosphere,Store in freezer, under -20°C
酸度系数(pKa)11.24±0.70(Predicted)
VU 0364770 用途与合成方法
生物活性VU0364770 是一种有效的选择性 mGlu4 正变构调节剂 (PAM)。VU0346770 对大鼠 mGlu4 和人 mGlu4 受体的 EC50 分别为 290 nM 和 1.1 μM。VU0364770 对 mGlu5 具有拮抗活性,EC50 为 17.9 μM,VU0364770 对 mGlu6 具有正变构调节活性,EC50 为 6.8 μM。VU0364770 还对 MAO 具有活性,作用于人 MAO-A 和 MAO-B 的 Ki 值分别为8.5 和 0.72 μM。
靶点

Rat mGlu 4

290 nM (EC 50 )

Human mGlu 4

1.1 μM (EC 50 )

mGlu 6

6.8 μM (EC 50 )

mGlu 5

17.9 μM (EC 50 )

体外研究

VU0364770 is a selective positive allosteric modulator of mGlu 4 in recombinant systems. VU0364770 is a potent PAM of multiple signaling pathways that enhances the response of the rat and human mGlu 4 receptors to the endogenous agonist glutamate. VU0364770 produces a concentration-dependent potentiation of the response to an EC 20 concentration of glutamate with EC 50 of 1.1±0.2 μM 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 IC 50 determinations is performed for VU0364770 at the MAO-A and MAO-B isoforms; these studies result in K i s of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively. When tested at a 10 μM 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 mGlu 4 at 10 μM). When further evaluated in a full concentration-response curve format, VU0364770 exhibits antagonist activity at mGlu 5 with a potency of 17.9±5.5 μM and PAM activity at mGlu 6 with a potency of 6.8±1.7 μM (compare with the potency of VU0364770 on the rat mGlu 4 receptor of 290±80 nM).

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 mGlu 4 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 (F 6,69 =8.04; p<0.001).

用途 N-(3-Chlorophenyl)-2-pyridinecarboxamide shows positive allosteric modulation at the mGlu4 receptors in combination with other antagonists resulting in treatment for the neurodegenerative Parkinson鈥檚 disease.
安全信息
VU 0364770 价格(试剂级)
更新日期产品编号产品名称CAS编号包装价格
2022/04/29HY-100588VU036477061350-00-35mg600元
2022/04/29HY-100588VU036477061350-00-310mg900元
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