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Art. -Nr.: HY-187840

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RBI257

RBI257 is a selective dopamine D4R antagonist with a pK_i of 8.42 for the hD4.4 receptor. RBI257 acts as a competitive antagonist at the hD4.4 receptor, blocking dopamine-stimulated G protein activation and GIRK current activation. RBI257 can be used for research on hypertension and schizophrenia.

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CAS. Nr.: 194038-94-3
Formel: C₂₁H₂₈IN₃O
Molecular Weight:465.38

Speicherung:

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

RBI257 Chemical Structure

CAS. Nr.: 194038-94-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
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- In Vitro
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Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

Human D₄ Receptor

8.42 (pKi)

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

RBI257 (10-100 μM) does not affect NHE activity in immortalized renal proximal tubular epithelial cells from SHR and WKY rats^[1].
RBI257 exhibits high affinity for the hD4.4 receptor in CHO-hD4.4 cell membranes (pK_i = 8.42)^[3].
RBI257 acts as an antagonist of the hD_4.4 receptor and exhibits potent antagonism of dopamine-stimulated [³⁵S]GTPγS binding, with pK_B values of 9.37 (30 mM NaCl) and 9.01 (100 mM NaCl)^[3].

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

Related Protocols :

Research Protocol for Cardiovascular Diseases

Chemical Information

CAS. Nr. 194038-94-3
Molecular Weight 465.38
Formel C₂₁H₂₈IN₃O
SMILES

IC1=CC=C(C=C1)CN2CCC(N(C3=NC=CC=C3OC(C)C)C)CC2
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

Handling Instructions (2659 KB)

Verweise

[1]. Pedrosa R, et al. Dopamine D3 receptor-mediated inhibition of Na+/H+ exchanger activity in normotensive and spontaneously hypertensive rat proximal tubular epithelial cells. British journal of pharmacology. 2004 Aug;142(8):1343-53.

[2]. Moran-Gates T, et al. Repeated antipsychotic drug exposure in developing rats: dopamine receptor effects. Synapse (New York, N.Y.). 2006 Feb;59(2):92-100.

[3]. Newman-Tancredi A, et al. Agonist and antagonist properties of antipsychotics at human dopamine D4.4 receptors: G-protein activation and K+ channel modulation in transfected cells. The international journal of neuropsychopharmacology. 2008 May;11(3):293-307.

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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RBI257

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Beschreibung

IC50 & Target

In Vitro

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

RBI257 Related Classifications

HY-187840 Related Classifications

Bioz

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