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VU6005649 Sale

目录号 : GC19381

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 Chemical Structure

Cas No.:2137047-43-7

规格 价格 库存 购买数量
1mg
¥262.00
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5mg
¥810.00
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10mg
¥1,350.00
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25mg
¥2,455.00
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50mg
¥5,850.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

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.

产品描述

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.

Chemical Properties

Cas No. 2137047-43-7 SDF
Canonical 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
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.7989 mL 13.9946 mL 27.9893 mL
5 mM 0.5598 mL 2.7989 mL 5.5979 mL
10 mM 0.2799 mL 1.3995 mL 2.7989 mL
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