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VU6005649

  Cat. No.:  DC10717   Featured
Chemical Structure
2137047-43-7
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More than 5000 active chemicals with high quality for research!
Field of application
VU6005649 is a dual mGlu7/8 positive allosteric modulator with EC50s of 649 nM and 2.6 μM for mGlu7 and mGlu8, respectively.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2137047-43-7
Chemical Name: 3-(2,3-Difluoro-4-methoxy-phenyl)-2,5-dimethyl-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine
Synonyms: VU6005649; VU-6005649; VU 6005649
SMILES: FC(C1=CC(C)=NC2=C(C3=CC=C(OC)C(F)=C3F)C(C)=NN12)(F)F
Formula: C16H12F5N3O
M.Wt: 357.28
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: 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.
Target: EC50: 0.65 μM (mGlu7 receptor ), 2.6 μM (mGlu8 receptor)[1]
In Vivo: 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].
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[1].
Animal Administration: 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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC10717 VU6005649 VU6005649 is a dual mGlu7/8 positive allosteric modulator with EC50s of 649 nM and 2.6 μM for mGlu7 and mGlu8, respectively.
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