VU 0361737 1161205-04-4

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Molecular Weight: 262.69 VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors, can penetrate into CNS.

Biological Activity

VU0361737 is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors
and displays weak activity at mGlu5 and mGlu8 receptors.


VU0361737 shows high in vivo CL in rat, a short half-life (T1/2 20 min), and demonstrates significant brain exposure (brain-to-plasma ratio of 4.1).





Protocol(Only for Reference)

Kinase Assay: [2]

Calcium mobilization assays

Human mGluR4/Gqi5/CHO cells (30,000 cells/20 •l/well) are plated in blackwalled, clear-bottomed, TC treated, 384 well plates in DMEM containing 10% dialyzed FBS, 20 mM HEPES, 100 units/ml penicillin/streptomycin, and 1 mM sodium pyruvate. The cells are grown overnight at 37 °C in the presence of 5% CO2. During the day of assay, the medium is replaced with 20 μL of 1 μM Fluo-4, AM prepared as a 2.3 mM stock in DMSO and mixed in a 1:1 ratio with 10% (w/v) pluronic acid F-127 and diluted in Assay Buffer (Hank`s balanced salt solution, 20 mM HEPES and 2.5 mM Probenecid) for 45 minutes at 37 °C. Dye is removed and replaced with 20 μL of Assay Buffer. Test compounds are transferred to daughter plates using an Echo acoustic plate reformatter and then diluted into Assay Buffer. Ca2+ flux is measured using the Functional Drug Screening System 6000. Baseline readings are taken (10 images at 1 Hz, excitation, 470±20 nm, emission, 540±30 nm) and then 20 •l/well test compounds are added using the FDSS`s integrated pipettor. Cells are incubated with compounds for approximately 2.5 minutes and then an EC20 concentration of glutamate is applied; 2 minutes later an EC80 concentration of glutamate is added. For concentration-response curve experiments, compounds are serially diluted 1:3 into 10 point concentration response curves and are transferred to daughter plates using the Echo. Test compounds are again applied and followed by EC20 concentrations of glutamate. For fold shift experiments, compounds are added at 2X their final concentration and then increasing concentrations of glutamate are added in the presence of vehicle or the appropriate concentration of test compound. Curves are fitted using a four point logistical equation using Microsoft XLfit. Subsequent confirmations of concentrationresponse parameters are performed using independent serial dilutions of source compounds and data from multiple days experiments are integrated and fit using a four point logistical equation in GraphPad Prism. Calcium assays are used to assess activity of compounds at mGluRs 1, 4 and 5.

Animal Study: [1]

Animal Models	Sprague-Dawley rats
Formulation	10% Tween-80
Dosages	10 mg/kg
Administration	ip

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	262.69
Formula	C13H11ClN2O2
CAS No.	1161205-04-4

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	53 mg/mL (201.75 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	2-Pyridinecarboxamide, N-(4-chloro-3-methoxyphenyl)-

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Product Categories : Neuronal Signaling > GluR Inhibitor