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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 628730-30-3
分子式: C₉H₁₂N₂S
分子量:180.27

保管条件:

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

AGN-201781 構造式

CAS 番号: 628730-30-3

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性

製品説明

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

Adrenergic Receptor アイソフォーム固有の製品をすべて表示 :

体外実験

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.

体内実験

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.

臨床実験

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

化学情報

CAS 番号 628730-30-3
分子量 180.27
分子式 C₉H₁₂N₂S
SMILES

S=C1NC=C(N1)CC2CC=CC2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Daniel W. Gil, et al. Compositions and their uses for alleviating pain. WO2003099289A2. 2003.

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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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