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VU0361737

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Purity:99.86%

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COA LCMS HNMR HPLC

VU0361737

Catalog No. T6726Cas No. 1161205-04-4

VU0361737 (ML-128) is a specific positive allosteric modulator (PAM) of the mGlu4 receptor with an EC50 of 240 nM for human receptors and 110 nM for rat receptors. It exhibits weak activity at mGlu5 and mGlu8 receptors and is inactive at mGlu1, mGlu2, mGlu3, mGlu6, and mGlu7 receptors. The compound can penetrate the CNS.

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Pack Size	Price	Availability
5 mg	$31	In Stock
10 mg	$48	In Stock
25 mg	$93	In Stock
50 mg	$156	In Stock
100 mg	$255	In Stock
500 mg	$626	In Stock
1 mL x 10 mM (in DMSO)	$35	In Stock

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Product Introduction

Bioactivity

Description	VU0361737 (ML-128) is a specific positive allosteric modulator (PAM) of the mGlu4 receptor with an EC50 of 240 nM for human receptors and 110 nM for rat receptors. It exhibits weak activity at mGlu5 and mGlu8 receptors and is inactive at mGlu1, mGlu2, mGlu3, mGlu6, and mGlu7 receptors. The compound can penetrate the CNS.
Targets&IC50	mGluR4 (rat):110 nM(EC50), mGluR4 (human):240 nM(EC50)
In vitro	VU0361737 is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. [1]
In vivo	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). [1]
Kinase Assay	Enzyme Assays: The enzymatic activities of NAMPT and NMNAT are measured using in vitro kits and using the Two-Step Method per manufacturer's instructions. Compounds, NAMPT and/or NMNAT enzymes, and their substrates are mixed and incubated at 30°C for 1 hour. Reagents for the indicator reaction (Wst-1) are then added, and absorbance is read at 450 nm every 5 min at 30°C on a Tecan In?nite M100 multimode plate reader.
Alias	ML-128, VU 0361737

Chemical Properties

Molecular Weight	262.69
Formula	C13H11ClN2O2
Cas No.	1161205-04-4

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 45 mg/mL (171.3 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.8068 mL	19.0338 mL	38.0677 mL	190.3384 mL
5 mM	0.7614 mL	3.8068 mL	7.6135 mL	38.0677 mL
10 mM	0.3807 mL	1.9034 mL	3.8068 mL	19.0338 mL
20 mM	0.1903 mL	0.9517 mL	1.9034 mL	9.5169 mL
50 mM	0.0761 mL	0.3807 mL	0.7614 mL	3.8068 mL
100 mM	0.0381 mL	0.1903 mL	0.3807 mL	1.9034 mL

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