VU6005649 是一种中枢神经系统渗透性的mGlu7/8受体激动剂，对于mGlu7受体和mGlu8受体的EC50分别为 0.65 μM 和 2.6 μM。
产品描述
VU6005649 is an agonist of CNS penetrant mGlu7/8 receptor (EC50s: 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively).
体外活性
VU6005649 is an agonist of CNS penetrant mGlu7/8 receptor(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.
体内活性
In wild-type mice VU6005649 shows modest but significant pro-cognitive effects on associative learning and the first example of efficacy of an mGlu7/8 positive allosteric modulator (PAM) in this model.
Cas No.
2137047-43-7
分子式
C16H12F5N3O
分子量
357.28
储存和溶解度
DMSO:60 mg/ml (167.94 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
