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Art. -Nr.: HY-151547

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MRS4719

MRS4719 is a potent P2X4 receptor antagonist with an IC₅₀ value of 0.503 μM for human P2X4 receptor. MRS4719 can reduce infarct volume and reduce brain atrophy, showing neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4719 also reduces ATP-induced [Ca²⁺]_i influx in primary human monocyte-derived macrophages. MRS4719 can be used to research ischemic stroke.

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CAS. Nr.: 2840581-32-8
Formel: C₂₆H₁₃N₅O₃S.C₆H₁₅N
Molecular Weight:504.60

Speicherung:

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

Data Sheet (280 KB)

MRS4719 Chemical Structure

CAS. Nr.: 2840581-32-8

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC₅₀: 0.503 μM (P2X4 receptor)^[1]

Alle P2X Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

MRS4719 (compound 21u) (0.1, 0.3, 0.6, 1.0 and 3.0 μM; 15 min) inhibits P2X4R-mediated Ca²⁺ influx in primary human monocyte-derived macrophages.^[1].

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

In Vivo

MRS4719 (compound 21u) (0.5-3 mg/kg; 3 days continuous infusion with an Alzet minipump) reduce infarct volume and reduced brain atrophy; does not improve motor coordination and balance as assessed using rotarod; improves learning and memory after stroke^[1].

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

Animal Model:

Male and female young C57B/6 mice (8-12 weeks; induced transient focal cerebral ischemia by a 60 min right middle cerebral artery occlusion)^[1]
Dosage:

0.5, 1.5 and 3 mg/kg
Administration:

3 days continuous infusion with an Alzet minipump
Result:

Caused significant neuroprotection using total hemispheric infarct volume size at doses 1.5 and 3.0 mg/kg.

Animal Model:

Middle-aged C57B/6 mice (11-12 month-old; induced transient focal cerebral ischemia by a 60 min right middle cerebral artery occlusion)^[1]
Dosage:

1.5 and 3 mg/kg
Administration:

3 days continuous infusion with an Alzet minipump
Result:

Did not improve motor coordination and balance as assessed using rotarod.

Animal Model:

Middle-aged C57B/6 mice (11-12 month-old; induced transient focal cerebral ischemia by a 60 min right middle cerebral artery occlusion)^[1]
Dosage:

3 mg/kg
Administration:

3 days continuous infusion with an Alzet minipump
Result:

Improved dose-dependently learning and memory after stroke and reached statistical significance at a dose of 3 mg/kg.

Chemical Information

CAS. Nr. 2840581-32-8
Molecular Weight 504.60
Formel C₂₆H₁₃N₅O₃S.C₆H₁₅N
SMILES

CC[NH+](CC)CC.O=C(NC1=C2C=CC=CC2=CC=C1N3C4=CC(C([N-]5)=NOC5=S)=NC=C4)CC3=O
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

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Toti KS, et al. Structure-Activity Relationship and Neuroprotective Activity of 1,5-Dihydro-2H-naphtho[1,2-b][1,4]diazepine-2,4(3H)-diones as P2X4 Receptor Antagonists. J Med Chem. 2022 Sep 23. [Content Brief]

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.

Keywords

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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MRS4719

Alle P2X Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

MRS4719 Related Classifications

HY-151547 Related Classifications