BMS309403

製品コード：S6622 純度：99.94%

BMS309403 is a small-molecule FABP4 inhibitor with nM affinity (Kd=4 nM for FABP4) and >100-fold selectivity against FABP5 as well as the heart isoform FABP3.

CAS No. 300657-03-8

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
25mg	JPY 55500	国内在庫あり
100mg	JPY 115500	国内在庫なし(納期7~10日)
1g	JPY 448500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（4）

製品安全説明書

現在のバッチを見る：純度： 99.94%

99.94

BMS309403関連製品

関連化合物ライブラリー	Metabolism Compound Library Anti-cancer Metabolism Compound Library Glutamine Metabolism Compound Library Carbohydrate Metabolism Compound Library Lipid Metabolism Compound Library	もっと見る

FABP阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
THP1	Function assay	25 uM	3 days	Reduction of transformation of human THP1 cells to foam cells at 25 uM after 3 days relative to control	17554340
aP2+/+ macrophage cells	Function assay	25 uM		Reduction in total cholesterol ester content in mouse aP2+/+ macrophage cells at 25 uM relative to control	17554340
aP2-/-R macrophage cells	Function assay	25 uM		Reduction in total cholesterol ester content in mouse aP2-/-R macrophage cells (re-expression of aP2) at 25 uM relative to control	17554340
THP1	Function assay	25 uM		Increase in APOA1-mediated cholesterol in human THP1 cells at 25 uM relative to control	17554340
THP1	Function assay	25 uM		Increase in ABCA1 mRNA level in human THP1 cells at 25 uM relative to control	17554340
THP1	Function assay	25 uM		Increase in ABCA1 protein level in human THP1 cells at 25 uM relative to control	17554340
aP2+/+ macrophage cells	Function assay	25 uM		Increase in cholesterol efflux in mouse aP2+/+ macrophage cells at 25 uM relative to control	17554340
aP2-/-R macrophage cells	Function assay	25 uM		Increase in cholesterol efflux in mouse aP2-/-R macrophage cells (re-expression of aP2) at 25 uM relative to control	17554340
aP2+/+ macrophage cells	Function assay		24 hrs	Decrease in MCP1 production in mouse aP2+/+ macrophage cells after 24 hrs	17554340
aP2-/-R macrophage cells	Function assay		24 hrs	Decrease in MCP1 production in mouse aP2-/-R macrophage cells (re-expression of aP2) after 24 hrs	17554340
BL21(DE3)	Function assay			Displacement of 1,8-ANS from His6-tagged FABP4 (unknown origin) expressed in Escherichia coli BL21(DE3) cells by fluorescence assay, Ki=0.22μM	27460668
BL21(DE3)	Function assay			Direct binding to His6-tagged FABP4 (unknown origin) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry, Kd=2.05μM	27460668
THP1	Function assay			Reduction of Mcp1 expression in human THP1 cells expressing aP2 relative to control	17554340
aP2+/+ macrophage cells	Function assay			Reduction of Mcp1 expression mouse aP2+/+ macrophage cells relative to control	17554340
aP2-/-R macrophage cells	Function assay			Reduction of Mcp1 expression mouse aP2-/-R macrophage cells (re-expression of aP2) relative to control	17554340
THP1	Function assay			Reduction of IL1-beta expression in human THP1 cells expressing aP2 relative to control	17554340
aP2+/+ macrophage cells	Function assay			Reduction of IL1-beta expressed in mouse aP2+/+ macrophage cells relative to control	17554340
aP2-/-R macrophage cells	Function assay			Reduction of IL1-beta expressed in mouse aP2-/-R macrophage cells (re-expression of aP2) relative to control	17554340
THP1	Function assay			Reduction of IL6 expression in human THP1 cells expressing aP2 relative to control	17554340
aP2+/+ macrophage cells	Function assay			Reduction of IL6 expression mouse aP2+/+ macrophage cells relative to control	17554340
aP2-/-R macrophage cells	Function assay			Reduction of IL6 expression mouse aP2-/-R macrophage cells (re-expression of aP2) relative to control	17554340
THP1	Function assay			Reduction of TNF expression in human THP1 cells expressing aP2 relative to control	17554340
aP2+/+ macrophage cells	Function assay			Reduction of TNF expression in mouse aP2+/+ macrophage cells relative to control	17554340
aP2-/-R macrophage cells	Function assay			Reduction of TNF expression mouse aP2-/-R macrophage cells (re-expression of aP2) relative to control	17554340
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生物活性

製品説明

BMS309403 is a small-molecule FABP4 inhibitor with nM affinity (Kd=4 nM for FABP4) and >100-fold selectivity against FABP5 as well as the heart isoform FABP3.

Targets

FABP4 ^[1]
(Cell-free assay)

4 nM(Kd)

In Vitro
In vitro	Treatment of BMS309403 (FABP4 inhibitor) comobined with SSO (CD36 inhibitor) significantly decreases the breast cancer cell viability, proliferative, migratory, and invasive abilities over 72 h. Inhibiting either at recommended concentrations does not significantly decrease the breast cancer cell viability over 72 h. Treatment with both SSO and BMS309403 results in clustering of cells and increased lipid content, indicating an inability to metabolise lipids resulting potentially in lipotoxicity-induced apoptosis.^[1]
細胞実験	細胞株	Humen breast cancer cell lines
	濃度	20 μM
	反応時間	72 h
	実験の流れ	Cell viability after CD36 knockout or treatment with SSO and BMS-309403 is determined by seeding 2500 cells in 96-well plate, and cultured for 24 h, after which treatment agent is added at appropriate concentration and maintained for 72 h. Cell viabilities is evaluated at 6, 12, 24, 36, 48, 60 and 72 h using the EZ-CYTOX cell viability kit.

In Vivo
In Vivo	Treatment with either BMS309403 or SSO alone decreases the rate of tumour formation and the combination of BMS309403 and SSO significantly decreased the rate of tumour formation.

参考
[1] Gyamfi J, et al. NPJ Breast Cancer. 2021 Sep 24;7(1):129. [2] Lan H, et al. J Lipid Res. 2011, 52(4):646-56.

参考

化学情報

分子量	474.55	化学式	C₃₁H₂₆N₂O₃
CAS No.	300657-03-8	SDF	--
Smiles	CCC1=C(C(=NN1C2=CC=CC=C2C3=CC(=CC=C3)OCC(=O)O)C4=CC=CC=C4)C5=CC=CC=C5
保管	3 years -20°C powder	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3 years -20°C powder	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 95 mg/mL ( (200.18 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 18 mg/mL

Water : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.					投与溶液組成計算機
	Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	6.0mg/ml (12.64mM)	Taking the 1 mL working solution as an example, add 50 μL of 120 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.	投与溶液組成計算機
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.75mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 95 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	0.475mg/ml (1.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 9.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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