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Basimglurant {[allProObj[0].p_purity_real_show]}

货号:A467450 同义名: CTEP Derivative;Rg7090 Ambeed 开学季,买赠积分,赢豪礼

RG7090 is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM.

Basimglurant 化学结构 CAS号:802906-73-6
Basimglurant 化学结构
CAS号:802906-73-6
Basimglurant 3D分子结构
CAS号:802906-73-6
Basimglurant 化学结构 CAS号:802906-73-6
Basimglurant 3D分子结构 CAS号:802906-73-6
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Basimglurant 纯度/质量文件 产品仅供科研

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Basimglurant 生物活性

描述 Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM[1].
体内研究

Basimglurant (RG7090) is a potent, selective, and safe mGlu5 inhibitor with good oral bioavailability and long half-life supportive of once-daily administration, good brain penetration, and high in vivo potency. Its ability to alleviate symptoms of depression is validated through functional magnetic resonance imaging (fMRI) assessments, alongside its capacity to produce anxiolytic-like and antinociceptive effects[1].

Basimglurant is undergoing phase II clinical trials for depression and fragile X syndrome treatment, Basimglurant consistently extends drinking time in the Vogel conflict drinking test in a dose-dependent manner. Effective doses of Basimglurant (RG7090) yield a plasma exposure range from 5 ng/mL (0.03 mg/kg) to 37 ng/mL (0.3 mg/kg)[2].

体外研究

Detailed analysis using [3H]-basimglurant on recombinant human mGlu5 receptors shows monophasic saturation isotherms with a Kd of 1.1 nM. In competitive binding assays, Basimglurant effectively displaces [3H]-MPEP and [3H]-ABP688 with Ki values of 35.6 nM and 1.4 nM, respectively. Moreover, in HEK293 cells expressing human mGlu5, it inhibits quisqualate-induced Ca2+ mobilization and [3H]-inositolphosphate accumulation with IC50 values of 7.0 nM and 5.9 nM, respectively. Its efficacies are consistent across both human and rodent mGlu5 receptor orthologues.

Basimglurant 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.

Basimglurant 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.07mL

0.61mL

0.31mL

15.35mL

3.07mL

1.53mL

30.70mL

6.14mL

3.07mL

Basimglurant 技术信息

CAS号802906-73-6
分子式C18H13ClFN3
分子量 325.767
别名 CTEP Derivative;Rg7090
运输蓝冰
存储条件

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 35 mg/mL(107.44 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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