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Tocris/VU 29/4458/10/10 mg

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货号: 4458/10

品牌: Tocris

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Description: Potent mGlu₅ allosteric potentiator

Chemical Name: N-(1,3-Diphenyl-1H-pyrazolo-5-yl)-4-nitrobenzamide

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent allosteric potentiator at the rat mGlu₅ receptor (EC₅₀ = 9 nM); binds to the MPEP (Cat. No. 1212) allosteric site (K_{i app} = 244 nM). Selective for mGlu5 over mGlu₁ and mGlu₂ receptors (EC₅₀ values are 557 nM and 1.51 μM for mGlu₁ and mGlu₂ respectively). Potentiates both DHPG-induced LTP and threshold θ-burst stimulation (TBS)-induced LTP in rat hippocampal slices. Analog of CDPPB (Cat. No. 3235).

Compound Libraries

VU 29 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	384.39
Formula	C₂₂H₁₆N₄O₃
Storage	Store at RT
Purity	≥99% (HPLC)
CAS Number	890764-36-0
PubChem ID	11610682
InChI Key	KIALCSMRIHRFPL-UHFFFAOYSA-N
Smiles	O=C(C4=CC=C([N+]([O-])=O)C=C4)NC1=CC(C3=CC=CC=C3)=NN1C2=CC=CC=C2

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
Solubility	DMSO	38.44	100

Preparing Stock Solutions

The following data is based on the product molecular weight 384.39. 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	2.6 mL	13.01 mL	26.02 mL
5 mM	0.52 mL	2.6 mL	5.2 mL
10 mM	0.26 mL	1.3 mL	2.6 mL
50 mM	0.05 mL	0.26 mL	0.52 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Chen et al (2007) Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses. Mol.Pharmacol. 71 1389 PMID: 17303702

de Paulis et al (2006) Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes. J.Med.Chem. 49 3332 PMID: 16722652

Ayala et al (2009) mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning. Neuropsychopharmacology 34 2057 PMID: 19295507

Keywords: VU 29, supplier, VU29, mGlu5, mGluR5, pams, positive, allosteric, potentiators, modulators, glutamate, receptors, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience

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