VU 0409551

Name: VU 0409551
Brand: Tocris Bioscience
SKU: 5693

Tocris Bioscience, part of Bio-Techne | Catalog # 5693

Citations (3)

COA / SDS

Selective positive allosteric modulator of mGlu5 receptors; brain penetrant and orally bioavailable

Key Product Details

Description:	Selective positive allosteric modulator of mGlu₅ receptors; brain penetrant and orally bioavailable
Alternative Names:	JNJ 46778212
Chemical Name:	[6,7-Dihydro-2-(phenoxymethyl)oxazolo[5,4-c]pyridin-5(4H)-yl](fluorophenyl)methanone
Purity:	≥98% (HPLC)
Molecular Weight:	352.36

View Full Technical Details for VU 0409551

Technical Data
Citations

Biological Activity for VU 0409551

VU 0409551 is a selective mGlu₅ positive allosteric modulator (EC₅₀ = 260 nM). Selective for mGlu₅ over other mGluR subtypes, as well as 66 other receptors and ion channels. Selectively potentiates mGlu₅ signaling via G_αq. Exhibits wake-promoting, antipsychotic-like and cognition-enhancing effects in animal models. Brain penetrant and orally available.

Compound Libraries for VU 0409551

VU 0409551 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for VU 0409551

M. Wt	352.36
Formula	C₂₀H₁₇FN₂O₃
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	1363281-27-9
PubChem ID	56846694
InChi Key	QUZLMKNNIUSREV-UHFFFAOYSA-N
Smiles	O=C(C1=CC=C(F)C=C1)N(C2)CCC3=C2OC(COC4=CC=CC=C4)=N3

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 0409551

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	35.24	100
	ethanol	17.62	50

Preparing Stock Solutions for VU 0409551

The following data is based on the product molecular weight 352.36.

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	2.84 mL	14.19 mL	28.38 mL
5 mM	0.57 mL	2.84 mL	5.68 mL
10 mM	0.28 mL	1.42 mL	2.84 mL
50 mM	0.06 mL	0.28 mL	0.57 mL

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References for VU 0409551

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

Conde-Ceide Discovery of VU0409551/JNJ-46778212: An mGlu₅ positive allosteric modulator clinical candidate targeting schizophrenia. ACS Med.Chem.Lett. 2015 PMID: 26157544
Ghoshal Role of mGlu5 receptors and inhibitory neurotransmission in M1 dependent muscarinic LTD in the prefrontal cortex: implications in Schizophrenia. ACS Chem.Neurosci. 2017 PMID: 28679049
Rook Biased mGlu₅-positive allosteric modulators provide in vivo efficacy without potentiating mGlu₅ modulation of NMDAR currents. Neuron 2015 PMID: 25937172