VU 0364770

Name: VU 0364770
Brand: Selleck Chemicals
SKU: S2862
Rating: 5 (0 reviews)

For research use only.

Catalog No.S2862

Molecular Weight(MW): 232.67

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

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Biological Activity

Description

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

Targets

mGlu4 ^[1]

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]

Protocol

Animal Research:^[1]	- Collapse Animal Models: Haloperidol-Induced Catalepsy Dosages: 1–56.6 mg/kg Administration: s.c. (Only for Reference)

References

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

Solubility (25°C)

In vitro	DMSO	47 mg/mL (202.0 mM)
	Ethanol	47 mg/mL (202.0 mM)
	Water	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 Information Download VU 0364770 SDF

Molecular Weight	232.67
Formula	C₁₂H₉ClN₂O
CAS No.	61350-00-3
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	ClC1=CC(=CC=C1)NC(=O)C2=NC=CC=C2

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Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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