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VU0361737

Catalog No. T6726 CAS 1161205-04-4

Synonyms: ML-128, VU 0361737

VU0361737 (ML-128) is a specific positive allosteric modulator (PAM) of mGlu4 receptor.The EC50 of VU 0361737 is 240 nM for the human receptors. The EC50 of VU 0361737 is110 nM for rat receptors.It exhibits weak activity at mGlu5 and mGlu8 receptors, and is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors, can penetrate into CNS.

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VU0361737, CAS 1161205-04-4

Pack Size	Availability	Price/USD
5 mg	In stock	$ 31.00
10 mg	In stock	$ 48.00
25 mg	In stock	$ 93.00
50 mg	In stock	$ 156.00
100 mg	In stock	$ 255.00
500 mg	In stock	$ 626.00
1 mL * 10 mM (in DMSO)	In stock	$ 35.00

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Purity: 99.86%

Purity: 99.09%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	VU0361737 (ML-128) is a specific positive allosteric modulator (PAM) of mGlu4 receptor.The EC50 of VU 0361737 is 240 nM for the human receptors. The EC50 of VU 0361737 is110 nM for rat receptors.It exhibits weak activity at mGlu5 and mGlu8 receptors, and is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors, can penetrate into CNS.
Targets&IC50	mGluR4 (human):240 nM(EC50), mGluR4 (rat):110 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.

Synonyms	ML-128, VU 0361737
Molecular Weight	262.69
Formula	C13H11ClN2O2
CAS No.	1161205-04-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (171.3 mM)

References and Literature

1. Engers DW, et al. J Med Chem, 2009, 52(14), 4115-4118. 2. Engers DW, et al. J Med Chem, 2011, 54(4), 1106-1110.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Membrane Protein-targeted Compound Library Anti-Parkinson's Disease Compound Library NO PAINS Compound Library Neurotransmitter Receptor Compound Library Neuronal Signaling Compound Library Bioactive Compound Library Glutamine Metabolism Compound Library Bioactive Compounds Library Max

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Keywords

VU0361737 1161205-04-4 Neuroscience GluR Parkinson's inhibit neuroprotective Metabotropic glutamate receptors ML-128 VU-0361737 VU 0361737 Inhibitor disease ML 128 mGluR ML128 inhibitor

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