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製品番号: HY-125089

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AM-643

AM-643 is a FLAP inhibitor with human IC₅₀ of 2 nM, oral activity, and dermal activity.AM-643 selectively inhibits FLAP, reduces leukotriene biosynthesis and reduces inflammatory ear swelling.AM-643 can be used for the research of skin disorders involving leukotriene production.

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: 1233114-22-1
分子式: C₃₆H₄₀N₄O₄S
分子量:624.80

保管条件:

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

AM-643 構造式

CAS 番号: 1233114-22-1

価格（税別）

Amount: USD 0.00

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Use of MCE Products

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

生物活性

製品説明

体外実験

AM-643 (compound 6) potently inhibits ³H-ligand binding to human polymorphonuclear leukocyte-derived FLAP membranes with an IC₅₀ of 2 nM^[1].
AM-643 potently inhibits calcium ionophore-induced LTB₄ synthesis in isolated human leukocytes with an IC₅₀ of 0.6 nM^[1].
AM-643 (15 min-5 h) inhibits calcium ionophore-induced LTB₄ synthesis in human whole blood with an IC₅₀ of 161 nM after 15 minutes of pre-incubation and an IC₅₀ of 81 nM after 5 hours of pre-incubation^[1].
AM-643 inhibits human CYP 3A4 with an IC₅₀ of 8.8 μM, human CYP 2C9 with an IC₅₀ of 4.5 μM, and does not inhibit human CYP 2D6 at concentrations up to 30 μM^[1].

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

体内実験

AM-643 (compound 6) (30 mg/kg; p.o.; single dose) produces a 65% inhibition of arachidonic acid-induced ear edema and a 57% reduction in CysLT concentrations in mouse ear tissue^[1].
AM-643 (0.01, 0.1%; topical; single dose) produces a 61% inhibition of arachidonic acid-induced ear edema, a 37% reduction in CysLT concentrations, and a 55% reduction in LTB₄ concentrations in mouse ear tissue in vivo in a concentration-dependent manner^[1].
AM-643 (10 mg/mL; topical; single dose; occluded for 24 hours) causes no dermal irritancy and results in detectable systemic exposure in abraded healthy male rats^[1].

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

化学情報

CAS 番号 1233114-22-1
分子量 624.80
分子式 C₃₆H₄₀N₄O₄S
SMILES

O=C(O)C(C)(C)CC1=C(SC(C)(C)C)C=2C=C(OCC3=NC=C(C=C3)C)C=CC2N1CC=4C=CC(=CC4)C5=NC=C(OC)C=N5
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]. Stock N, et al. 5-Lipoxygenase-activating protein inhibitors. Part 3: 3-{3-tert-Butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM643)—A potent FLAP inhibitor suitable for topical administration. Bioorganic & Medicinal Chemistry Letters, 2010, 20(15): 4598-4601.

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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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