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VU0364770

Catalog No. T6727 CAS 61350-00-3

Synonyms: VU 0364770

VU0364770 (VU 0364770)(EC50=1.1 μM), a positive allosteric modulator(PAM) of mGlu4, shows insignificant activity at 68 other receptors, including other mGlu subtypes.

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VU0364770, CAS 61350-00-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 48.00
10 mg	In stock	$ 74.00
25 mg	In stock	$ 93.00
50 mg	In stock	$ 166.00
100 mg	In stock	$ 263.00
1 mL * 10 mM (in DMSO)	In stock	$ 108.00

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Purity: 99.92%

Purity: 99.66%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	VU0364770 (VU 0364770)(EC50=1.1 μM), a positive allosteric modulator(PAM) of mGlu4, shows insignificant activity at 68 other receptors, including other mGlu subtypes.
Targets&IC50	mGlu4:1.1 μM(EC50)
In vitro	VU0364770 is a potent and effective positive allosteric modulator of mGlu4. VU0346770 exhibits a potency of 1.1 ± 0.2 μM at human mGlu4 in the presence of an EC20 concentration of glutamate and shifts the glutamate concentration-response curve 31.4 ± 4.0-fold to the left. VU0364770 exhibits a potency of 290 ± 80 nM at rat mGlu4 and induces an 18.1 ± 1.7-fold left shift of the glutamate concentration-response curve. [1]
In vivo	VU0364770 shows efficacy alone or when administered in combination with l-DOPA or an adenosine 2A (A2A) receptor antagonist preladenant currently in clinical development. When administered alone, VU0364770 exhibits efficacy in reversing haloperidol-induced catalepsy, forelimb asymmetry-induced by unilateral 6-hydroxydopamine (6-OHDA) lesions of the median forebrain bundle, and attentional deficits induced by bilateral 6-OHDA nigrostriatal lesions in rats. In addition, VU0364770 enhances the efficacy of preladenant to reverse haloperidol-induced catalepsy when given in combination. The effects of VU0364770 to reverse forelimb asymmetry are also potentiated when the compound is coadministered with an inactive dose of l-DOPA, suggesting that mGlu4 positive allosteric modulator may provide l-DOPA-sparing activity. [1]
Kinase Assay	The effects of VU0364770 on rat mGlu1 and mGlu5 are assessed by using calcium mobilization and measuring the glutamate concentration-response relationship in the presence and absence of 10 μM VU0364770. Using a double-addition protocol, VU0364770 is added to the cells, followed 2.5 min later by a full concentration-response of glutamate. Shifts of the concentration-response relationship are used to assess potential potentiator (left shift of more than 2-fold) or antagonist (right shift of more than 2-fold or depression of the maximum response by at least 75%) activity of VU0364770. Compounds are further assessed for mGlu5 antagonist activity by performing a full concentration-response curve, starting at 30 μM and serially diluted it by using 1:3 dilutions, in the presence of an EC80 concentration of glutamate[1].

Synonyms	VU 0364770
Molecular Weight	232.67
Formula	C12H9ClN2O
CAS No.	61350-00-3

Storage

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

Solubility Information

DMSO: 23.3 mg/mL (100 mM)

References and Literature

1. Jones CK, et al. J Pharmacol Exp Ther, 2012, 340(2), 404-421.

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 Glutamine Metabolism Compound Library NO PAINS Compound Library Bioactive Compounds Library Max

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Keywords

VU0364770 61350-00-3 Neuroscience GluR inhibit Metabotropic glutamate receptors VU-0364770 Inhibitor VU 0364770 mGluR inhibitor

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