VU 0364770 - Moligand™, 10mM in DMSO , Allosteric modulator of mGlu 4 receptor, CAS No.61350-00-3, Allosteric modulator of mGlu 4 receptor

CAS: 61350-00-3 Cat. No.: V408226 Peso molecular: 232.67 Número EC: 111-965-3 PubChem CID: 836002

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

2-Pyridinecarboxamide, N-(3-chlorophenyl)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

VU 0364770 is a positive allosteric modulator(PAM) ofmGlu4withEC50of 1.1 μM, exhibits insignificant activity at 68 other receptors, including other mGlu subtypes.
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.

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.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

2-Pyridinecarboxamide, N-(3-chlorophenyl)-

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

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.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Grado

Moligand™

Tipo de acción

ALLOSTERIC MODULATOR

Mecanismo de acción

Allosteric modulator of mGlu 4 receptor

Nombres e identificadores

• Isómeros SMILES: C1=CC=NC(=C1)C(=O)NC2=CC(=CC=C2)Cl
• CAS alternativo: 61350-00-3
• PubChem CID: 836002
• Términos de entrada MeSH: N-(3-chlorophenyl)picolinamide;VU0364770
• Peso molecular: 232.67

Objetivos asociados (humanos)

GRM4 Tchem Metabotropic glutamate receptor 4 (2 Activities)

Discover Target: GRM4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 58 mg/mL (199.45 mM); Ethanol: 58 mg/mL (199.45 mM); Water: Insoluble