VU-29 is a PAM (positive allosteric modulator) of the metabotropic glutamate 5 (mGlu5) receptor (EC50=9 nM, Ki=244 nM for rmGluR5). VU-29 is selective for mGluR5 relative to other isoforms (EC50= rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM).

Physicochemical Properties

Molecular Formula	C22H16N4O3
Molecular Weight	384.39
Exact Mass	384.122
CAS #	890764-36-0
PubChem CID	11610682
Appearance	Light yellow to yellow solid powder
LogP	5.296
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	4
Heavy Atom Count	29
Complexity	561
Defined Atom Stereocenter Count	0
InChi Key	KIALCSMRIHRFPL-UHFFFAOYSA-N
InChi Code	InChI=1S/C22H16N4O3/c27-22(17-11-13-19(14-12-17)26(28)29)23-21-15-20(16-7-3-1-4-8-16)24-25(21)18-9-5-2-6-10-18/h1-15H,(H,23,27)
Chemical Name	N-(2,5-diphenylpyrazol-3-yl)-4-nitrobenzamide
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	rat mGluR5 9 nM (EC50) rat mGluR1 557 nM (EC50) rat mGluR2 1.5 μM (EC50) hmGluR4 154 nM (EC50) rat mGluR5 224 nM (Ki)
ln Vivo	In rat hippocampal slices, VU-29 (500 nM) amplifies the effects of DHPG on phosphoinositide (PI)-induced hydrolysis. In the rat hippocampus CA1 area, VU-29 enhances threshold TBS-induced long term potentiation (LTP). In rat hippocampal region CA1, VU-29 (1 µM) enhances chemically induced mGluR-long term depression (LTD). VU-29 (1 µM) enhances NMDA receptor-independent LTD caused by stimuli[1].
References	[1]. mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning. Neuropsychopharmacology. 2009;34(9):2057-2071. [2]. 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. 2007;71(5):1389-1398.

Solubility Data

Solubility (In Vitro)

DMSO: 50 mg/mL (130.08 mM)

Solubility (In Vivo)

Solubility in Formulation 1: 5 mg/mL (13.01 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.6015 mL	13.0076 mL	26.0152 mL
	5 mM	0.5203 mL	2.6015 mL	5.2030 mL
	10 mM	0.2602 mL	1.3008 mL	2.6015 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.