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抑制剂描述:

产品名称:VU 0364770

产品别名:见爱必信官网

英文别名:VU 0364770

靶点:mGluR

CAS:61350-00-3

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

VU 0364770是一种mGlu4正变构调节剂(PAM),EC50为1.1 μM,对68种其他受体,包括其他mGlu亚型,几乎没有作用活性。VU0364770是一种强有效的代谢型谷氨酸受体4 (mGlu4)正向别构调节剂。在含有EC20浓度谷氨酸盐情况下1.1 μM的VU0346770 对人源mGlu4效能可以使谷氨酸盐浓度响应曲线向左移动31.4倍。290 nM的 VU0364770对大鼠mGlu4具有效能并诱导谷氨酸盐浓度响应曲线向左移动18.1 倍。

溶解性:DMSO :23.3 mg/mL (100 mM)

体外研究:

VU0364770 is a potent and effective positive allosteric modulator of mGlu4. VU0346770 exhibits a potency of 1.1 ± 0.2 μM at human mGlu4 in the presence of an EC20 concentration of glutamate and shifts the glutamate concentration-response curve 31.4 ± 4.0-fold to the left. VU0364770 exhibits a potency of 290 ± 80 nM at rat mGlu4 and induces an 18.1 ± 1.7-fold left shift of the glutamate concentration-response curve.

体内研究:VU0364770 shows efficacy alone or when administered in combination with l-DOPA or an adenosine 2A (A2A) receptor antagonist preladenant currently in clinical development. When administered alone, VU0364770 exhibits efficacy in reversing haloperidol-induced catalepsy, forelimb asymmetry-induced by unilateral 6-hydroxydopamine (6-OHDA) lesions of the median forebrain bundle, and attentional deficits induced by bilateral 6-OHDA nigrostriatal lesions in rats. In addition, VU0364770 enhances the efficacy of preladenant to reverse haloperidol-induced catalepsy when given in combination. The effects of VU0364770 to reverse forelimb asymmetry are also potentiated when the compound is coadministered with an inactive dose of l-DOPA, suggesting that mGlu4 positive allosteric modulator may provide l-DOPA-sparing activity.

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