规格

价格

库存

数量

2 mg

¥ 128

现货

5 mg

¥ 202

现货

10 mg

¥ 300

现货

25 mg

¥ 386

现货

50 mg

¥ 691

现货

100 mg

¥ 1,080

现货

500 mg

¥ 2,500

现货

1 mL x 10 mM (in DMSO)

¥ 209

现货

生物活性

产品描述	VU0364770 (VU 0364770)(EC50=1.1 μM), a positive allosteric modulator(PAM) of mGlu4, shows insignificant activity at 68 other receptors, including other mGlu subtypes.
靶点活性	mGlu5:17.9 μM (EC50), mGlu6:6.8 μM (EC50), mGlu4:1.1 μM (EC50)
体外活性	VU0364770是一种有效的mGlu4正向异构调节剂，显示出在EC20浓度的谷氨酸存在下，对人mGlu4的潜力为1.1 ± 0.2 μM，并将谷氨酸浓度-反应曲线向左移动31.4 ± 4.0倍。在大鼠mGlu4上，VU0364770展示出290 ± 80 nM的活性，并促使谷氨酸浓度-反应曲线左移18.1 ± 1.7倍。[1]
体内活性	VU0364770单独使用或与l-DOPA或正在临床开发中的腺苷2A（A2A）受体拮抗剂preladenant合用时显示出疗效。单独使用时，VU0364770能有效逆转由haloperidol引起的僵直、由单侧6-羟基多巴胺（6-OHDA）损伤造成的前肢不对称性以及由双侧6-OHDA损害黑质-纹状体引起的注意力缺陷。此外，与preladenant联合使用时，能增强逆转haloperidol引起的僵直症状。当VU0364770与无活性剂量的l-DOPA联合给药时，可以增强逆转前肢不对称性的效果，这表明mGlu4正向异构调节剂可能具有节省l-DOPA用量的活性。[1]
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 10 μM 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 30 μM and serially diluted it by using 1:3 dilutions, in the presence of an EC80 concentration of glutamate[1].
别名	VU 0364770

化学信息

分子量	232.67
分子式	C₁₂H₉ClN₂O
CAS No.	61350-00-3
Smiles	Clc1cccc(NC(=O)c2ccccn2)c1
密度	1.341 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

实际储存温度请以COA为准

溶解度信息

DMSO: 50 mg/mL (214.9 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (8.6 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	4.2979 mL	21.4897 mL	42.9793 mL	214.8966 mL
5 mM	0.8596 mL	4.2979 mL	8.5959 mL	42.9793 mL
10 mM	0.4298 mL	2.1490 mL	4.2979 mL	21.4897 mL
20 mM	0.2149 mL	1.0745 mL	2.1490 mL	10.7448 mL
50 mM	0.0860 mL	0.4298 mL	0.8596 mL	4.2979 mL
100 mM	0.0430 mL	0.2149 mL	0.4298 mL	2.1490 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

VU0364770

VU0364770

产品介绍

引用文献

计算器

体内实验配液计算器

剂量转换

关键词

VU0364770

VU0364770

VU0364770 相关产品

产品介绍

引用文献

计算器

体内实验配液计算器

剂量转换

关键词