Tocris/VU 0409551/5693/10/10 mg-蚂蚁淘生物

Description: Selective mGlu₅ positive allosteric modulator; 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) Biological Activity Technical Data Solubility Calculators DatasheetsReferences

Biological Activity

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.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM Solubility

DMSO	35.24	100
ethanol	17.62	50

Preparing Stock Solutions

The following data is based on the product molecular weight 352.36. Batch specific molecular weights may vary from batch to batch due to solvent 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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Product Datasheets

Certificate of Analysis / Product Datasheet Safety Datasheet Select another language: English German French Spanish View SDS

References

References are publications that support the products\' biological activity.

Rook et al (2015) Biased mGlu₅-positive allosteric modulators provide in vivo efficacy without potentiating mGlu₅ modulation of NMDAR currents. Neuron 86 1029 PMID: 25937172

Conde-Ceide et al (2015) Discovery of VU0409551/JNJ-46778212: An mGlu₅ positive allosteric modulator clinical candidate targeting schizophrenia. ACS Med.Chem.Lett. 6 716 PMID: 26157544

Keywords: VU 0409551, supplier, JNJ46778212, VU0409551, metabotropic, glutamate, receptors, mGlu5, positive, allosteric, modulators, modulates, PAMs, JNJ, 46778212, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience