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Art. -Nr.: HY-100323

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AGN-201781

AGN-201781 is an orally active α-2B adrenergic receptor agonist. AGN-201781 can be used in studies related to neuropathic pain.

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CAS. Nr.: 628730-30-3
Formel: C₉H₁₂N₂S
Molecular Weight:180.27

Speicherung:

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

AGN-201781 Chemical Structure

CAS. Nr.: 628730-30-3

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Use of MCE Products

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

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

Biologische Aktivität

Beschreibung

AGN-201781 is an orally active α-2B adrenergic receptor agonist. AGN-201781 can be used in studies related to neuropathic pain^[1].

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

AGN-201781 (compound 11) acts as a potent α-2B-preferring adrenergic agonist with no detectable activity at α-2A receptors, weak activity at α-2C receptors, minimal activity at α-1A receptors, and no activity at α-1B or α-1D receptors^[1].

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

In Vivo

AGN-201781 (compound 11) (30-1000 μg/kg; p.o.; single dose; 0.1 mg/kg/hour; subcutaneous osmotic minipump; continuous; 5 days) produces significant acute neuropathic pain relief at oral doses of 100 μg/kg and higher, and maintains ~80% allodynia reversal for at least 30 days following 5 days of continuous subcutaneous administration^[1].
AGN-201781 (1 mg/kg; i.p.; single dose; 0.5 mg/kg; i.v.; single dose; 3 mg/kg; p.o.; single dose) does not produce significant sedative or cardiovascular side effects at doses higher than those required for peak neuropathic pain relief in rats^[1].

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

Animal Model:

Sprague-Dawley (male, 100-120 grams for acute dosing; neuropathic pain Chung model via partial ligation of left spinal nerves L-5 and L-6)^[1]
Dosage:

30-1000 μg/kg (acute oral); 0.1 mg/kg/hour (extended subcutaneous)
Administration:

p.o.; single dose (acute); subcutaneous osmotic minipump; continuous; 5 days (extended)
Result:

Produced no significant allodynia reversal at 30 μg/kg.
Produced 60-90% peak allodynia reversal at 100 μg/kg and 300 μg/kg, with effects diminishing by 140 minutes post-dose.
Produced lower peak allodynia reversal at 1000 μg/kg, with effects diminishing over time.
Achieved ~80% allodynia reversal during 5-day continuous dosing, with analgesic effect maintained at the same level for 30 days post-dosing.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 628730-30-3
Molecular Weight 180.27
Formel C₉H₁₂N₂S
SMILES

S=C1NC=C(N1)CC2CC=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]. Daniel W. Gil, et al. Compositions and their uses for alleviating pain. WO2003099289A2. 2003.

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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MOQ

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100 mg

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