VU6005649
目录号: PL07144 纯度: ≥99%
CAS No. :2137047-43-7
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中文名称
VU6005649
中文别名
3-(2,3-二氟-4-甲氧基苯基)-2,5-二甲基-7-(三氟甲基)-吡唑并[1,5-a]嘧啶;化合物 T13321
英文名称
VU6005649
英文别名
VU 6005649;VU6005649;VU-6005649; VU-6005649; VU 6005649;CS-2729;Pyrazolo[1,5-a]pyrimidine, 3-(2,3-difluoro-4-methoxyphenyl)-2,5-dimethyl-7-(trifluoromethyl)-
Cas No.
2137047-43-7
分子式
C16H12F5N3O
分子量
357.28
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
VU6005649 是一个 CNS 渗透性的 mGlu7/8 受体激动剂,对于 mGlu7 受体和 mGlu8 受体的 EC50 值分别为 0.65 μM 和 2.6 μM。
生物活性
VU6005649 is a CNS penetrant mGlu 7/8 receptor agonist with EC 50 s of 0.65 μM and 2.6 μM for mGlu 7 receptor and mGlu 8 receptor, respectively.
性状
Solid
IC50 & Target[1][2]
mGlu7 Receptor 0.65 μM (EC50) mGlu8 Receptor
体外研究(In Vitro)
VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM 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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
When VU6005649 (compound 9f) is dosed at 30 mg/kg IP in 10% Tween 80/H 2 O (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 mGlu 7/8 positive allosteric modulator (PAM) in this model. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 50 mg/mL (139.95 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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