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VU0360172

Catalog No. T29126 CAS 1310012-12-4

Synonyms: VU-0360172, VU 0360172

VU0360172 is a positive allosteric modulator of mGlu5 receptors (EC50 = 16 nM; Ki = 195 nM).

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VU0360172, CAS 1310012-12-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 74.00
5 mg	In stock	$ 178.00
10 mg	In stock	$ 289.00
25 mg	In stock	$ 592.00
50 mg	In stock	$ 853.00
100 mg	In stock	$ 1,180.00
1 mL * 10 mM (in DMSO)	In stock	$ 167.00

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Purity: 99.65%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	VU0360172 is a positive allosteric modulator of mGlu5 receptors (EC50 = 16 nM; Ki = 195 nM).
Targets&IC50	mGlu5:16 nM(EC50), mGlu5:195 nM(Ki)
In vivo	VU0360172 stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice[4].

Synonyms	VU-0360172, VU 0360172
Molecular Weight	294.32
Formula	C18H15FN2O
CAS No.	1310012-12-4

Storage

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

Solubility Information

DMSO: 83 mg/mL (282.01 mM), Sonication is recommended.

References and Literature

1. Notartomaso S, Mascio G, Scarselli P, Martinello K, Fucile S, Gradini R, Bruno V, Battaglia G, Nicoletti F. Expression of the K(+)/Cl(-) cotransporter, KCC2, in cerebellar Purkinje cells is regulated by group-I metabotropic glutamate receptors. Neuropharmacology. 2017 Mar 15;115:51-59. doi: 10.1016/j.neuropharm.2016.07.032. Epub 2016 Aug 3. PubMed PMID: 27498071. 2. Sengmany K, Singh J, Stewart GD, Conn PJ, Christopoulos A, Gregory KJ. Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery. Neuropharmacology. 2017 Mar 15;115:60-72. doi: 10.1016/j.neuropharm.2016.07.001. Epub 2016 Jul 5. PubMed PMID: 27392634; PubMed Central PMCID: PMC5217481. 3. D'Amore V, Raaijmakers RH, Santolini I, van Rijn CM, Ngomba RT, Nicoletti F, van Luijtelaar G. The anti-absence effect of mGlu5 receptor amplification with VU0360172 is maintained during and after antiepileptogenesis. Pharmacol Biochem Behav. 2016 Jul-Aug;146-147:50-9. doi: 10.1016/j.pbb.2016.05.004. Epub 2016 May 10. PubMed PMID: 27178815. 4. Kiritoshi T, Ji G, Neugebauer V. Rescue of Impaired mGluR5-Driven Endocannabinoid Signaling Restores Prefrontal Cortical Output to Inhibit Pain in Arthritic Rats. J Neurosci. 2016 Jan 20;36(3):837-50. doi: 10.1523/JNEUROSCI.4047-15.2016. PubMed PMID: 26791214; PubMed Central PMCID: PMC4719019.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Anti-Neurodegenerative Disease Compound Library Neurotransmitter Receptor Compound Library Bioactive Compound Library Neuronal Signaling Compound Library Bioactive Compounds Library Max

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Keywords

VU0360172 1310012-12-4 Neuroscience GluR CD1 mice Metabotropic glutamate receptors VU-0360172 Polyphosphoinositide Inhibitor PI hydrolysis mGluR inhibit VU 0360172 inhibitor

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