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Basimglurant

Basimglurant (CTEP Derivative) 是一种高效，选择性，可口服的 mGlu5负变构调节剂，Kd 值为1.1 nM。

CAS号

802906-73-6

分子式

C18H13ClFN3

主要靶点

GluR

仅限科研使用

Cat No : CM05099

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Synonyms

CTEP Derivative|RG7090

验证数据展示

  • CAS No.: 802906-73-6

    Basimglurant
    CAS#: 802906-73-6

产品信息

Basimglurant is a potent, selective and orally available modulator of mGlu5 negative allosteric(Kd of 1.1 nM).

CAS号 802906-73-6
分子式 C18H13ClFN3
主要靶点 GluR
主要通路 神经科学
分子量 325.77
纯度 99.38%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 CTEP Derivative|RG7090

靶点活性

mGlu5 Receptor:1.1 nM (Kd)

体内活性

Basimglurant is selective and safe inhibitor of mGlu5 with good oral bioavailability and long half-life supportive of once-daily administration, good brain penetration, and high in vivo potency. Basimglurant has antidepressant properties which are corroborated by its functional magnetic imaging (fMRI) profile, as well as anxiolytic-like and antinociceptive features[1].

体外活性

In competition binding experiments on human recombinant mGlu5, Basimglurant (RG7090) fully displaces [3H]-MPEP with a Ki of 35.6 nM and [3H]-ABP688 with a Ki of 1.4 nM. In HEK293 cells stably expressing human mGlu5, Basimglurant (RG7090) inhibits quisqualate induced Ca2+ mobilization with an IC50 of 7.0 nM and [3H]-inositolphosphate accumulation (IC50 of 5.9 nM). Basimglurant shows similar potencies in radioligand binding and functional assay on human and rodent mGlu5 receptor orthologues[1].

溶解度

DMSO:33.33 mg/mL (102.31 mM)

参考文献

1.Lindemann L, et al. Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression. J Pharmacol Exp Ther. 2015 Apr;353(1):213-33.
2.Jaeschke G, et al. Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases.

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