Basimglurant RG7090; CTEP Derivative|cas:802906-73-6|西域试剂

Basimglurant RG7090; CTEP Derivative,98.0%

产品编号：Bellancom-15446| CAS NO：802906-73-6| 分子式：C₁₈H₁₃ClFN₃| 分子量：325.77

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货号	价格	库存与货期
Bellancom-15446	￥3500.00	杭州北京（现货）
Bellancom-15446	￥5000.00	杭州北京（现货）
Bellancom-15446	￥0.00	杭州北京（现货）
Bellancom-15446	￥0.00	杭州北京（现货）

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Basimglurant RG7090; CTEP Derivative

产品介绍

Basimglurant (RG7090) 是高效，选择性有口服活性的mGlu5负变构调节剂，K_d值为1.1 nM。

生物活性

Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a K_d of 1.1 nM.

体外研究

[³H]-basimglurant saturation analysis on recombinant human mGlu5 reveals monophasic saturation isotherms with K_d of 1.1 nM. In competition binding experiments on human recombinant mGlu5, Basimglurant (RG7090) fully displaces [³H]-MPEP with a K_i of 35.6 nM and [³H]-ABP688 with a K_i 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 with an IC₅₀ of 5.9 nM. Basimglurant (RG7090) shows similar potencies in radioligand binding and functional assay on human and rodent mGlu5 receptor orthologues.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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. It has antidepressant properties which are corroborated by its functional magnetic imaging (fMRI) profile, as well as anxiolytic-like and antinociceptive features. It is currently in phase II clinical studies for the treatment of depression and fragile X syndrome. In the Vogel conflict drinking test, Basimglurant dose dependently increases the drinking time. The total plasma exposure of efficacious doses of Basimglurant (RG7090) ranges from 5 ng/mL (0.03 mg/kg) to 37 ng/mL (0.3 mg/kg).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 33.33 mg/mL (102.31 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0697 mL	15.3483 mL	30.6965 mL
5 mM	0.6139 mL	3.0697 mL	6.1393 mL
10 mM	0.3070 mL	1.5348 mL	3.0697 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (7.67 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.67 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (7.67 mM); Suspended solution; Need ultrasonic and warming

此方案可获得 2.5 mg/mL (7.67 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.67 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.67 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。