2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. Ro4491533

Ro4491533 is a selective, negative allosteric mGluR2/3 receptor modulator that is equally effective on both subtypes. Ro4491533 can completely block glutamate-induced calcium mobilization and glutamate-induced [35S]GTPγS binding accumulation. Ro4491533 has good pharmacokinetic properties in mice and rats, high oral bioavailability, and can pass through the blood-brain barrier. Ro4491533 can also reverse the motor inhibition effect of LY379268 in mice and show antidepressant activity in the forced swim test and tail suspension test.

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Ro4491533

Ro4491533 Chemische Struktur

CAS. Nr. : 579482-31-8

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Ro4491533 Related Antibodies

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Alle mGluR Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

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Beschreibung

Ro4491533 is a selective, negative allosteric mGluR2/3 receptor modulator that is equally effective on both subtypes. Ro4491533 can completely block glutamate-induced calcium mobilization and glutamate-induced [35S]GTPγS binding accumulation. Ro4491533 has good pharmacokinetic properties in mice and rats, high oral bioavailability, and can pass through the blood-brain barrier. Ro4491533 can also reverse the motor inhibition effect of LY379268 in mice and show antidepressant activity in the forced swim test and tail suspension test.

Cellular Effect
Cell Line Type Value Description References
CHO IC50
0.003 μM
Compound: 7am
Antagonist activity at recombinant rat mGluR2 expressed in forskolin-stimulated CHO cells assessed as inhibition of (1S,3R)-ACPD induced cAMP production
Antagonist activity at recombinant rat mGluR2 expressed in forskolin-stimulated CHO cells assessed as inhibition of (1S,3R)-ACPD induced cAMP production
[PMID: 20971004]
CHO IC50
0.014 μM
Compound: 7am
Antagonist activity at human mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current
Antagonist activity at human mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current
[PMID: 20971004]
CHO IC50
< 0.01 μM
Compound: 7am
Antagonist activity at rat mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current
Antagonist activity at rat mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current
[PMID: 20971004]
CHO IC50
< 0.01 μM
Compound: 7am
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
[PMID: 20971004]
Molekulargewicht

423.43

Formel

C24H20F3N3O
CAS. Nr.
SMILES

O=C1NC2=CC(C(F)(F)F)=C(C=C2N=C(C1)C3=CC=CC(C4=CC(C)=NC(C)=C4)=C3)C
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
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Ro4491533 Related Classifications

  • Molaritätsrechner

  • Verdünnungsrechner

Die Formel zur Berechnung von Molaritäten

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)

Diese Gleichung wird häufig abgekürzt als: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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.

Keywords:

Ro4491533579482-31-8Ro 4491533Ro-4491533mGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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