AICAR (Acadesine)

製品コードS1802 バッチS180207

化学情報

	Synonyms	NSC105823, AICA Riboside	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₉H₁₄N₄O₅
	分子量	258.23	CAS No.	2627-69-2
Solubility (25°C)*	体外	DMSO	51 mg/mL (197.49 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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.
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]
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]
特徴	A potential first-in-class ARA.

プロトコル(参考用のみ)

細胞アッセイ	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.
動物実験	動物モデル	mouse xenograft model of K562 cells
	投薬量	50 mg/kg
	投与方法	Injected intraperitoneally

参考

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カスタマーフィードバック

: , , British Journal of Pharmacology, 2015, 172(13):3284–3301.

: , , J Appl Toxicol, 2017, 37(10):1219-1224

: Data from [Data independently produced by , , J Clin Invest, 2019, 129(1):252-267]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Nuclear PD-L1 compartmentalization suppresses tumorigenesis and overcomes immunocheckpoint therapy resistance in mice via histone macroH2A1 [ J Clin Invest, 2024, 134(22)e181314]	PubMed: 39545415
PRMT5 mediated FUBP1 methylation accelerates prostate cancer progression [ J Clin Invest, 2024, e175023]	PubMed: 39146021
Brain Short-Chain Fatty Acids Induce ACSS2 to Ameliorate Depressive-Like Behavior via PPARγ-TPH2 Axis [ Research (Wash D C), 2024, 7:0400]	PubMed: 38939042
Aerobic exercise suppresses CCN2 secretion from senescent muscle stem cells and boosts muscle regeneration in aged mice [ J Cachexia Sarcopenia Muscle, 2024, 15(5):1733-1749]	PubMed: 38925632
Metabolic regulation of misfolded protein import into mitochondria [ Elife, 2024, 12RP87518]	PubMed: 38900507
Artemisinin conferred cytoprotection to human retinal pigment epithelial cells exposed to amiodarone-induced oxidative insult by activating the CaMKK2/AMPK/Nrf2 pathway [ J Transl Med, 2024, 22(1):844]	PubMed: 39285426
Molecular mechanism underlying miR-204-5p regulation of adipose-derived stem cells differentiation into cells from three germ layers [ Cell Death Discov, 2024, 10(1):95]	PubMed: 38388551
Forchlorfenuron-Induced Mitochondrial Respiration Inhibition and Metabolic Shifts in Endometrial Cancer [ Cancers (Basel), 2024, 16(5)976]	PubMed: 38473335
Rap1GAP exacerbates myocardial infarction by regulating the AMPK/SIRT1/NF-κB signaling pathway [ Cell Signal, 2024, 117:111080]	PubMed: 38320624
AMP-dependent kinase stimulates the expression of αKlotho [ FEBS Open Bio, 2024, 10.1002/2211-5463.13872]	PubMed: 39090792

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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