VU 6005649

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Cat.No. 6893 - VU 6005649 | C16H12F5N3O | CAS No. 2137047-43-7
Description: Positive allosteric modulators of mGlu7 and mGlu8 receptors; also NK1 antagonist; brain penetrant
Chemical Name: 3-(2,3-Difluoro-4-methoxyphenyl)-2,5-dimethyl-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (8)

Biological Activity

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

Technical Data

M. Wt 357.28
Formula C16H12F5N3O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2137047-43-7
PubChem ID 131954513
InChI Key NYBZCKAQIIPSDS-UHFFFAOYSA-N
Smiles COC1=C(F)C(F)=C(C=C1)C1=C2N=C(C)C=C(N2N=C1C)C(F)(F)F

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 35.73 100
ethanol 17.86 50

Preparing Stock Solutions

The following data is based on the product molecular weight 357.28. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.8 mL 13.99 mL 27.99 mL
5 mM 0.56 mL 2.8 mL 5.6 mL
10 mM 0.28 mL 1.4 mL 2.8 mL
50 mM 0.06 mL 0.28 mL 0.56 mL

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References

References are publications that support the biological activity of the product.

Abe et al (2017) Discovery of VU6005649, a CNS penetrant mGlu7/8 receptor PAM derived from a series of pyrazolo[1,5-a]pyrimidines. ACS.Med.Chem.Lett. 8 1110 PMID: 29057060


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