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製品番号: HY-135495

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AM-0466

AM-0466 is a sodium channel inhibitor with nanomolar levels of NaV1.7 inhibitory activity. AM-0466 exhibits potent pharmacodynamic activity in a NaV1.7-dependent histamine-induced itch model. AM-0466 also showed significant analgesic effects in capsaicin-induced pain models. After optimizing its pharmacokinetic properties, AM-0466 was advanced into in vivo targeting and efficacy models for testing.

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: 1642113-59-4
分子式: C₂₇H₁₉F₃N₄O₄S
分子量:552.52

保管条件:

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

Data Sheet (272 KB)

AM-0466 構造式

CAS 番号: 1642113-59-4

容量

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Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

生物活性

製品説明

Sodium Channel アイソフォーム固有の製品をすべて表示 :

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

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	>30 μM Compound: 39	Inhibition of human Nav1.5 expressed in HEK293 cells incubated for 3 to 5 mins at -50 mV holding potential by patchXpress electrophysiology assay Inhibition of human Nav1.5 expressed in HEK293 cells incubated for 3 to 5 mins at -50 mV holding potential by patchXpress electrophysiology assay	[PMID: 28324649]
HEK293	IC₅₀	>42.5 μM Compound: 39	Inhibition of human Nav1.1 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay Inhibition of human Nav1.1 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay	[PMID: 28324649]
HEK293	IC₅₀	>42.5 μM Compound: 39	Inhibition of human Nav1.4 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay Inhibition of human Nav1.4 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay	[PMID: 28324649]
HEK293	IC₅₀	>42.5 μM Compound: 39	Inhibition of human Nav1.5 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay Inhibition of human Nav1.5 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay	[PMID: 28324649]
HEK293	IC₅₀	0.005 μM Compound: 2	Inhibition of slow inactivated human NaV1.7 expressed in HEK293 cells at -20 mV holding potential after 5 mins by IonWorks electrophysiology method Inhibition of slow inactivated human NaV1.7 expressed in HEK293 cells at -20 mV holding potential after 5 mins by IonWorks electrophysiology method	[PMID: 28684121]
HEK293	IC₅₀	0.006 μM Compound: 39	Inhibition of human Nav1.7 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay Inhibition of human Nav1.7 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay	[PMID: 28324649]
HEK293	IC₅₀	0.02 μM Compound: 2	Inhibition of human NaV1.7 expressed in HEK293 cells at -125 mV holding potential yielding 20 to 50% inactivation after 3 to 5 mins by PatchXpress automated electrophysiology method Inhibition of human NaV1.7 expressed in HEK293 cells at -125 mV holding potential yielding 20 to 50% inactivation after 3 to 5 mins by PatchXpress automated electrophysiology method	[PMID: 28684121]
HEK293	IC₅₀	0.021 μM Compound: 39	Inhibition of human Nav1.7 expressed in HEK293 cells at holding potential yielding 20 to 50% inactivation measured after 3 to 5 mins by patchXpress electrophysiology assay Inhibition of human Nav1.7 expressed in HEK293 cells at holding potential yielding 20 to 50% inactivation measured after 3 to 5 mins by patchXpress electrophysiology assay	[PMID: 28324649]
HEK293	IC₅₀	0.65 μM Compound: 39	Inhibition of human Nav1.6 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay Inhibition of human Nav1.6 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay	[PMID: 28324649]

化学情報

CAS 番号 1642113-59-4
分子量 552.52
分子式 C₂₇H₁₉F₃N₄O₄S
SMILES

O=C1N(C2=C(OC)C=C(C=C2)C3=CC(C(F)(F)F)=CC=C3)C4=CC=C(S(=O)(NC5=NC=CC=N5)=O)C=C4C=C1
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

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (272 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[1]. Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity

Calculators

モル濃度計算機

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

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希釈計算機

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濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

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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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参考文献

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AM-0466

Sodium Channel アイソフォーム固有の製品をすべて表示

Histamine Receptor アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

AM-0466 関連分類

HY-135495 関連分類