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Ro 67-4853
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ro 67-4853图片
CAS NO:302841-89-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
Ro 67-4853 是mGluR1的正向变构调节剂 (PAM),对于 rmGlu1a 受体的pEC50为7.16。Ro67-4853在包括 hmGlu1、rmGlu1 和 rmGlu5 在内的所有I 型 mGlu 受体上显示活性。Ro 67-4853 通过与受体的跨膜结构域 (TMD) 相互作用增强L-谷氨酸的效力。Ro 67-4853 增强对重复振动刺激的感觉突触反应。
生物活性

Ro 67-4853 is a positive allosteric modulator (PAM) ofmGluR1(pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation[1][2][3][4].

IC50& Target[1]

Rat mGluR1a

7.16 (pEC50)

体外研究
(In Vitro)

Ro67-4853 selectively potentiates responses to the agonist DHPG[2].
Ro 67-4853 (1 μM) shifts the concentration-response curve (CRC) of glutamate approximately 2-fold, 15-fold, and 4.5-fold to the left respectively in BHK cells stably expressing mGluR1a[4].
Ro 67-4853 (1 μM) activates p-ERK1/2 in the absence of agonist with a time course of activation peaking at 5 minutes in BHK cells[4].
Ro 67-4853 (500 nM) potentiates glutamate-induced activation of mGluR1 as assessed by measures of cAMP production. Glutamate increases cAMP accumulation with an EC50 value of 32.08 μM in the absence of Ro 67-4853. The EC50 values for glutamate in the presence of Ro 67-4853 is 2.15 μM. Ro 67-4853 increases basal mGluR1-induced cAMP accumulation and potentiate glutamate-induced cAMP accumulation but have lower potencies at modulating the cAMP response than at regulating ERK1/2 phosphorylation or calcium mobilization[4].

分子量

325.36

Formula

C19H19NO4

CAS 号

302841-89-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.