AICAR (Acadesine)

別名：NSC105823, AICA Riboside

製品コード：S1802 純度：99.97%

AICAR (Acadesine, NSC105823, AICA Riboside), an AMPK activator, results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. AICAR (Acadesine) induces mitophagy. Phase 3.

CAS No. 2627-69-2

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
50mg	JPY 22000	国内在庫あり
200mg	JPY 40500	国内在庫あり
500mg	JPY 58500	国内在庫あり
1g	JPY 100500	国内在庫あり

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（156）

製品安全説明書

現在のバッチを見る：純度： 99.97%

99.97

AICAR (Acadesine)と併用されることが多い化合物

Tanespimycin (17-AAG)

AICAR and 17-AAG treatment reduces cell proliferation and affects chromosome segregation in MEFs and human cancer cells.

Tang YC, et al. Cell. 2011 Feb 18; 144(4): 499–512.

Nutlin-3a

Nutlin-3a shows no synergistic activity with acadesine as it induces p53-independent apoptosis.

Coll-Mulet L, et al. Blood. 2006 May 15;107(10):4109-14.

AICAR (Acadesine)関連製品

関連ターゲット	AMPK-related protein kinase	もっと見る
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関連化合物ライブラリー	Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library	もっと見る

シグナル伝達経路

AMPKシグナル伝達経路

AMPK阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
3T3L1	Function assay	500 μM	5 h	Activation of AMPK in mouse 3T3L1 cells assessed as AMPK phosphorylation at 500 uM after 5 hrs by Western blotting analysis	25262940
3T3L1	Function assay	0.2 mM	9 days	Increase in AMPKalpha Thr172 phosphorylation in mouse 3T3L1 cells at 0.2 mM after 9 days by Western blot method	26088335
C2C12	Function assay	1 mM	1 hr	Activation of AMPK in mouse C2C12 cells assessed as increase in ACC phosphorylation at Ser79 residues at 1 mM after 1 hr by Western blot analysis	27887844
3T3L1	Function assay	2 mM	4 hrs	Induction of AMPKalpha phosphorylation at Thr172 residue in mouse 3T3L1 cells at 2 mM after 4 hrs by Western blot analysis	29425817
C2C12	Function assay	0.2 mM	30 mins	Inhibition of PTP1B in differentiated mouse C2C12 cells assessed as upregulation of ACC phosphorylation at Ser-79 residue at 0.2 mM after 30 mins by Western blot assay	28951079
RCC4	Function assay	1 mM	48 hrs	Induction of autophagy in human RCC4 cells assessed as increase in LC3 conversion at 1 mM after 48 hrs by Western blot method	28325600
3T3L1	Function assay	0.2 mM	3 days	Reduction in SCD1 protein expression in mouse 3T3L1 cells at 0.2 mM after 3 days by Western blot method	26088335
3T3L1	Function assay	0.2 mM	3 days	Reduction in SREBP-1c protein expression in mouse 3T3L1 cells at 0.2 mM after 3 days by Western blot method	26088335
3T3L1	Function assay	0.2 mM	9 days	Activation of AMPK in mouse 3T3L1 cells assessed as increase in ACC Ser79 phosphorylation at 0.2 mM after 9 days by Western blot method	26088335
3T3L1	Function assay	0.2 mM	3 days	Reduction in C/EBPalpha protein expression in mouse 3T3L1 cells at 0.2 mM after 3 days by Western blot method	26088335
3T3L1	Function assay	0.2 mM	3 days	Reduction in PPARgamma protein expression in mouse 3T3L1 cells at 0.2 mM after 3 days by Western blot method	26088335
3T3L1	Function assay	0.2 mM	3 days	Reduction in FAS protein expression in mouse 3T3L1 cells at 0.2 mM after 3 days by Western blot method	26088335
3T3L1	Function assay	0.2 mM		Inhibition of adipogenesis in mouse 3T3L1 cells assessed as reduction in triglyceride content at 0.2 mM by colorimetric assay	26088335
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生物活性

製品説明

特性

A potential first-in-class ARA.

Targets

AMPK ^[1]
(Cell-free assay)

AMPKK ^[1]
(Cell-free assay)

In Vitro
In vitro	Acadesine (500 μM) increases the ZMP content in extracts of isolated hepatocytes after up to 30-40 min treatment, then remains fairly constant at approximately 4 nmol/g. Acadesine (500 μM) causes a transient 12-fold activation of AMPK at 15 min in rat hepatocytes and 2-3 fold activation of AMPK in adipocytes, without affecting levels of ATP, ADP or AMP. Acadesine (500 μM) causes a dramatic inhibition of both fatty acid and sterol synthesis in rat hepatocytes. Acadesine (500 μM) also causes a dramatic inactivation of HMG-CoA reductase. ^[1] Acadesine induces apoptosis of B-CLL cells in a dose-dependent manner with EC50 of 380 μM. Acadesine (0.5 mM) decreases cell viability of B-CLL cells from 20 representative patients from 68% to 26%. Acadesine (0.5 mM) induces caspase activation and cytochrome crelease from mitochondria. Uptake and phosphorylation of Acadesine (0.5 mM) are required to induce apoptosis and activate AMPK in B-CLL cells. Acadesine (2-4 mM) only slightly affects the viability of T cells from B-CLL patients, Acadesine (0.5 mM) remarkedly reduces viability of B cells but not T cells. [2] Acadesine triggers loss of cell metabolism in K562, LAMA-84 and JURL-MK1 and is also effective in killing resistant K562 cells and Ba/F3 cells carrying the T315I-BCR-ABL mutation. The effect of Acadesine is abrogated by GF109203X and Ro-32-0432, both inhibitor of classical and new PKCs and accordingly, Acadesine triggers relocation and activation of several PKC isoforms in K562 cells. Acadesine dose-dependently inhibits K562 colony formation at day 10, the growth inhibitory effect of acadesine is already detected at 0.25 mM and is maximal at 2.5 mM. ^[3] Acadesine causes a concentration-related reduction in CD18 expression on LPS-stimulated neutrophils in vitro. ^[4] Acadesine significantly (1 mM) inhibits N-formyl-methionyl-leucyl-phenylalanine-induced granulocyte CD11b up-regulation by a mean of 61% in blood. ^[5]
細胞実験	細胞株	K562 cell lines
	濃度	2.5 mM
	反応時間	10 days
	実験の流れ	Acadesine is added to K562 cell lines or primary cells (10³ CD34+ cells/mL) growing in semisolid methyl cellulose medium. MethoCult H4100 or H4236 are used for cell lines and primary CD34+ cells respectively. Colonies are detected after 10 days of culture by adding 1 mg/mL of the MTT reagent and are scored by Image J quantification software.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	p-S6K1 / S6K1 / p-ERK / ERK p-IRS-1 / IRS-1 / p-AKT / AKT p-AMPK / p-ACC / p-eNOS / eNOS / vWF / VE-cadherin / ICAM-1 Cyclin D1 / p21 / p53		26528831
	Immunofluorescence	p-ERK YAZ / TAZ		26528831

In Vivo
In Vivo	Acadesine (50 mg/kg) significantly reduces tumor formation in a mouse xenograft model of K562 cells. ^[3] Acadesine (10 mg/kg) results in higher fluid required to stabilize hemodynamics in pigs. Acadesine (10 mg/kg) inhibits LPS-induced protein permeability of pulmonary capillaries, peak inspiratory pressures on constant tidal volume and dead space ventilation in pigs. ^[4]
動物実験	動物モデル	mouse xenograft model of K562 cells
	投与量	50 mg/kg
	投与経路	Injected intraperitoneally

参考
[1] Corton JM, et al. Eur J Biochem, 1995, 229(2), 558-565. [2] Campàs C, et al. Blood, 2003, 101(9), 3674-368 [3] Robert G, et al. PLoS One, 2009, 4(11), e7889. [4] Fabian TC, et al. Surgery, 1996, 119(3), 302-315. [5] Mathew JP, et al. J Thorac Cardiovasc Surg, 1995, 109(3), 448-456. + 展開

参考

+ 展開

化学情報

分子量	258.23	化学式	C₉H₁₄N₄O₅
CAS No.	2627-69-2	SDF	Download AICAR (Acadesine) SDFをダウンロードする
Smiles	C1=NC(=C(N1C2C(C(C(O2)CO)O)O)N)C(=O)N
保管	3年-20°C粉	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年-20°C粉	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ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 51 mg/mL ( (197.49 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。)

Water : 20 mg/mL

Ethanol : 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

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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