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VU 6005649

Cat. No. 6893 Submit a Review Datasheet / COA / SDS
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Description: Positive allosteric modulator 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 (3)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for VU 6005649

VU 6005649 is a 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.

Compound Libraries for VU 6005649

VU 6005649 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for VU 6005649

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 for VU 6005649

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

Preparing Stock Solutions for VU 6005649

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.

Select a batch to recalculate based on the batch molecular weight:
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 for VU 6005649

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

If you know of a relevant reference for VU 6005649, please let us know.

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Keywords: VU 6005649, VU 6005649 supplier, VU6005649, positive, allosteric, modulators, modulates, PAM, metabotropic, glutamate, receptor, 7, 8, group, III, mGlu, neurokinin, 1, antagonists, antagonism, tachykinin, NK1, Glutamate, (Metabotropic), Group, Receptors, Receptor, 6893, Tocris Bioscience

Citations for VU 6005649

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Metabotropic Glutamate Receptors Scientific Review

Metabotropic Glutamate Receptors Scientific Review

Written by Francine Acher, this review discusses the pharmacology and therapeutic potential of mGlu receptors, and the compounds acting upon them; compounds available from Tocris are listed.

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