VU0364770 HCl is a potent and specific mGlu4 PAM (positive allosteric modulator). VU0346770 HCl has EC50 of 290 nM and 1.1 μM for rat mGlu4 and human mGlu4 receptors, respectively. VU0364770 HCl has antagonistic activity against mGlu5 with EC50 of 17.9 μM, and VU0364770 HCl has positive allosteric modulating activity against mGlu6 with EC50 of 6.8 μM. VU0364770 HCl is also active against MAO, with Kis of 8.5 and 0.72 μM for human MAO-A and MAO-B, respectively.

Physicochemical Properties

Molecular Formula	C12H10CL2N2O
Molecular Weight	269.1266
Exact Mass	268.017
CAS #	1414842-70-8
Related CAS #	VU0364770;61350-00-3
PubChem CID	56587900
Appearance	Light yellow to yellow solid powder
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	2
Rotatable Bond Count	2
Heavy Atom Count	17
Complexity	247
Defined Atom Stereocenter Count	0
SMILES	ClC1=C([H])C([H])=C([H])C(=C1[H])N([H])C(C1=C([H])C([H])=C([H])C([H])=N1)=O.Cl[H]
InChi Key	CZNNJOSFWZBQKH-UHFFFAOYSA-N
InChi Code	InChI=1S/C12H9ClN2O.ClH/c13-9-4-3-5-10(8-9)15-12(16)11-6-1-2-7-14-11;/h1-8H,(H,15,16);1H
Chemical Name	N-(3-chlorophenyl)pyridine-2-carboxamide;hydrochloride
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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
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 mGlu4 290 nM (EC50) Human mGlu4 1.1 μM (EC50) mGlu6 6.8 μM (EC50) mGlu5 17.9 μM (EC50)
References	[1]. The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease. J Pharmacol Exp Ther.

Solubility Data

Solubility (In Vitro)

DMSO: 100 mg/mL (371.57 mM) H2O: < 0.1 mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 5 mg/mL (18.58 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. 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. Solubility in Formulation 2: ≥ 5 mg/mL (18.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 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 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.7157 mL	18.5784 mL	37.1568 mL
	5 mM	0.7431 mL	3.7157 mL	7.4314 mL
	10 mM	0.3716 mL	1.8578 mL	3.7157 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.