阿卡地新磷酸鹽作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetAICAR phosphateCat. No.: HY-13417ACAS No.: 681006-28-0分式: CHNOP分量: 356.23作靶點(diǎn): AMPK; Autophagy; Mitophagy作通路: Epigenetics; PI3K/Akt/mTOR; Autophagy儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) H2O : 180 mg/mL (505.29 mM)DMSO : 75 mg/mL (210.54 mM)*

2、means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 2.8072 mL 14.0359 mL 28.0718 mL5 mM 0.5614 mL 2.8072 mL 5.6143 mL10 mM 0.2807 mL 1.4036 mL 2.8072 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，

3、-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.84 mM); Clear solution此案

4、可獲得 2.08 mg/mL (5.84 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.84 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.08 mg/mL (5.84 mM，飽和度

5、未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.84 mM); Clear solution此案可獲得 2.08 mg/mL (5.84 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTI

6、VITY物活性 AICAR phosphate (Acadesine phosphate)種腺苷類似物，也 種 AMPK 激活劑。AICAR phosphate 調(diào)節(jié)葡萄糖和脂質(zhì)的代謝，并抑制促炎細(xì)胞因和 iNOS 的產(chǎn)。AMPK 激活劑。IC & Target AMPK Autophagy Mitophagy體外研究 HepG2 cells are treated with various concentrations of AICAR (0.1-1.0 mM) for 12, 24, and 48 h, respectively. Theexpression level of IR- si

7、gnificantly decreases with 0.25, 0.5, and 1.0 mM of AICAR at 48 h to 50%, 53%, and 46% ofthe control, respectively1.體內(nèi)研究 Fourteen-week-old male, lean (L; 31.3 g body wt) wild-type andob/ob (O; 59.6 g body wt) mice are injected with theAMP-activated kinase (AMPK) activator AICAR (A) at 0.5 mg*g body

8、wt-1*day-1 or saline control (C) for 14 days. At 24h after the last injection (including a 12-h fast), all mice are killed, and the plantar flexor complex muscle(gastrocnemius, soleus, and plantaris) is excised for analysis. Muscle mass is lower in OC (15912 mg) than LC, LA, andOA (17610, 1789, and

9、16616 mg, respectively) mice, independent of a body weight change3. The kidney weightis significantly higher in the untreated group when compared with both the exercise and AICAR (0.5 mg/g body wt)groups. The heart weight is higher in the exercise group than in the other groups, whereas the liver we

10、ight issignificantly higher in the AICAR-treated group when compared with the exercise and untreated groups4.PROTOCOLCell Assay 1 HepG2 cells (5105 cells) are plated in 6-well culture plate dishes and then are incubated in the serum-free media for12 h before transfection. One microgram of plasmid is

11、 transfected with FuGENE6 Transfection Reagent. After 5 h oftransfection, the culture media are removed and then media supplemented with or without AICAR (0.1-1.0 mM) areadded to each well. The stimulation media are changed every 24 h1.MCE has not independently confirmed the accuracy of these method

12、s. They are for reference only.Animal Mice2Administration 23 Fourteen-week-old lean (Lepob/+ or Lepob/+) and ob/ob (Lepob/Lepob/) male mice are uesd. After the 14-dayexperimental treatment (24 h after AICAR injection, including a 12-h fast), the plantar flexor complex muscle is cleanly(tendon-to-ten

13、don) excised from an anesthetized mouse. The muscle is quickly weighed and then processed forhistology or frozen in liquid nitrogen and stored at -80C. The anesthetized mice are killed by transection of thediaphragm and removal of the entire heart, after blood collection via needle puncture directly

14、 into the heart. AICARor saline (control) is injected subcutaneously into the lateral distal portion of the back. AICAR is administered at 0.5mg*g body wt-1*day-1 one time per day for 14 days. Saline (control) is injected in volumes identical to those used forAICAR treatment in a manner identical to

15、 that of AICAR treatment. Body weight is measured prior to death.Rats3Male 5-week-old ZDF rats are either subcutaneously injected with a single dose of AICAR (0.5 mg/g body wt) orPage 2 of 3 www.MedChemEunderwent a single bout of treadmill running (60 min, speed of 25 m/min at a 5% incline). Untreat

16、ed ZDF rats serveas controls (n=5 in each group). One hour after the subcutaneous AICAR injection or immediately after treadmillrunning, rats are killed by cervical dislocation. To avoid any effect of muscle spasm and hypoxia, red and whitegastrocnemius muscles are removed within seconds and immedia

17、tely freeze clamped for later determination ofAMPK activity.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cell Metab. 2019 Jul 2;30(1):157-173.e7 Oncogene. 2019 Sep;38(38):6537-6549. Cell Death Dis. 2018 May 1;9(5):515. Arch Toxicol. 2019

18、Jun;93(6):1697-1712. J Cell Physiol. 2018 Dec;233(12):9701-9715.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Nakamaru K, et al. AICAR, an activator of AMP-activated protein kinase, down-regulates the IR expression in HepG2 cells. Biochem Biophys ResCommun. 2005 Mar 11;328(2):449-542. Drake JC, et al. AICAR treatment for 14 days normalizes obesity-induced dysregulation of TORC1 signaling and translational capacity in fasted skeletalmuscle. Am J Physi