1. GPCR/G Protein Neuronal Signaling
  2. mGluR
  3. Ro 67-4853

Ro 67-4853 

Cat. No.: HY-107506
Handling Instructions

Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation.

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Ro 67-4853 Chemical Structure

Ro 67-4853 Chemical Structure

CAS No. : 302841-89-0

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Description

Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation[1][2][3][4].

IC50 & Target[1]

Rat mGluR1a

7.16 (pEC50)

In Vitro

Ro67-4853 selectively potentiates responses to the agonist DHPG[2].
Ro 67-4853 (1 µM) shifts the concentration-response curve (CRC) of glutamate approximately 2-fold, 15-fold, and 4.5-fold to the left respectively in BHK cells stably expressing mGluR1a[4].
Ro 67-4853 (1 µM) activates p-ERK1/2 in the absence of agonist with a time course of activation peaking at 5 minutes in BHK cells[4].
Ro 67-4853 (500 nM) potentiates glutamate-induced activation of mGluR1 as assessed by measures of cAMP production. Glutamate increases cAMP accumulation with an EC50 value of 32.08 µM in the absence of Ro 67-4853. The EC50 values for glutamate in the presence of Ro 67-4853 is 2.15 µM. Ro 67-4853 increases basal mGluR1-induced cAMP accumulation and potentiate glutamate-induced cAMP accumulation but have lower potencies at modulating the cAMP response than at regulating ERK1/2 phosphorylation or calcium mobilization[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

325.36

Formula

C19H19NO4

CAS No.
SMILES

CCCCOC(NC(C1C2=CC=CC=C2OC3=CC=CC=C13)=O)=O

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Ro 67-4853 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Ro 67-4853
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HY-107506
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