GlpBio

VU6005649

目录号: GC19381纯度: >98.50%
VU6005649 是一种 CNS 渗透性 mGlu7/8 受体激动剂，对 mGlu7 受体和 mGlu8 受体的 EC50 分别为 0.65 μM 和 2.6 μM。
VU6005649
Cas No.: 2137047-43-7
规格价格库存数量操作
1mg¥279.00现货
1
5mg¥630.00现货
1
10mg¥990.00现货
1
25mg¥1,782.00现货
1
50mg¥2,610.00现货
1
100mg¥3,780.00现货
1
10mM (in 1mL DMSO)¥495.00现货
1
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文献被引

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    641, 529–536 (2025)
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    610, 366–372 (2022)
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    187(9):2288-2304 (2024)
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    183(7):1867-1883 (2020)
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产品描述 Description

VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 uM and 2.6 uM for mGlu7 receptor and mGlu8 receptor, respectively.

VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 uM and 2.6 uM for mGlu7 receptor and mGlu8 receptor, respectively. VU6005649 displays a terminal Kp of 2.43 with total brain levels ~9× above the mGlu7 positive allosteric modulator (PAM) in vitro EC50[1].

When VU6005649 (compound 9f) is dosed at 30 mg/kg IP in 10% Tween 80/H2O (0.75 mg/kg. s.c. amphetamine), no efficacy is observed in this assay. VU6005649 shows modest but significant pro-cognitive effects on associative learning in wild-type mice and the first example of efficacy of an mGlu7/8 positive allosteric modulator (PAM) in this model[1].

References:
[1]. Abe M, et al. Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines. ACS Med Chem Lett. 2017 Sep 1;8(10):1110-1115.

实验参考方法 Experimental Reference Method

Animal experiment:

Tissue distribution studies with VU6005649 (compound 9f) in mice are performed by formulating VU6005649 in 10% polysorbate 80 and dosing via intraperitoneal injection to 20 week old female C57/Bl6 mice (3 per time point). At 0.25, 0.5, 1, 3, and 6 hours post dose, animals are euthanized and decapitated, blood is collected via cardiac puncture and the brains are removed, thoroughly washed in cold phosphate-buffered saline, and immediately frozen on dry ice[1].

References:

[1]. Abe M, et al. Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines. ACS Med Chem Lett. 2017 Sep 1;8(10):1110-1115.

产品文档 Product Documents

Purity:>98.50%

化学性质Chemical Properties

CAS 号
2137047-43-7
SMILES
CC1=NN2C(N=C(C)C=C2C(F)(F)F)=C1C3=CC=C(OC)C(F)=C3F
分子式
C16H12F5N3O
分子量
357.28 g/mol
溶解性
DMSO : 50 mg/mL (139.95 mM; Need ultrasonic)
保存条件
Store at -20°C
General tips
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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol