VU 6005649

Name: VU 6005649
Brand: Tocris Bioscience
SKU: 6893

Tocris Bioscience, part of Bio-Techne | Catalog # 6893

COA / SDS

Positive allosteric modulator of mGlu7 and mGlu8 receptors; also NK1 antagonist; brain penetrant

Key Product Details

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)
Molecular Weight:	357.28

View Full Technical Details for VU 6005649

Technical Data
Citations

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 mGlu_1,2,3,4,5,6). Also NK₁ receptor antagonist (K_i= 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 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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.80 mL	13.99 mL	27.99 mL
5 mM	0.56 mL	2.80 mL	5.60 mL
10 mM	0.28 mL	1.40 mL	2.80 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 Discovery of VU6005649, a CNS penetrant mGlu_7/8 receptor PAM derived from a series of pyrazolo[1,5-a]pyrimidines. ACS.Med.Chem.Lett. 2017 PMID: 29057060