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468780 VU 6005649 CAS: 2137047-43-7

Specifications
References
CAS Number
2137047-43-7
Grade
Highly Purified
Molecular Formula
C₁₆H₁₂F₅N₃O
Molecular Weight
357.28
EU Commodity Code
38220090
Shipping Temp
RT
Storage Temp
-20°C
3-(2,3-Difluoro-4-methoxyphenyl)-2,5-dimethyl-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine

VU 6005649 is a positive allosteric modulator of mGlu7 and mGlu8 receptors (EC50 = 0.65uM and 2.6uM for mGlu7 and mGlu8, respectively). Displays >3.8 fold selectivity for mGlu7 and mGlu8 over other mGlu receptors (EC50 >10uM for mGlu1,2,3,4,5,6). Also NK1 receptor antagonist (Ki= 650 nM, IC50 = 3.4uM). Brain penetrant.

Synonyms
3-(2,3-Difluoro-4-methoxyphenyl)-2,5-dimethyl-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine
CAS No
2137047-43-7
Molecular Formula
C₁₆H₁₂F₅N₃O
Molecular Weight
357.28
Solubility
100mM in DMSO and to 50mM in ethanol
Purity
≥98%
Appearance
Yellow solid
1H NMR and MS
Consistent with structure
Storage and Stability
Store at -20°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
References
1. Discovery of VU6005649, a CNS penetrant mGlu7/8 receptor PAM derived from a series of pyrazolo[1,5-a]pyrimidines. Abe et al. ACS.Med.Chem.Lett., 2017;8:1110
USBio References
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