1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAICAR phosphateCat. No.: HY-13417ACAS No.: 681006-28-0Synonyms: Acadesine phosphate; AICA Riboside phosphate分式: CHNOP分量: 356.23作靶點: AMPK; Autophagy; Mitophagy作通路: Epigenetics; PI3K/Akt/mTOR; Autophagy儲存式: Powder -20C 3 years4C 2

2、 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 H2O : 180 mg/mL (505.29 mM)DMSO : 75 mg/mL (210.54 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)

3、產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.84 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (

4、20% SBE-CD in saline)1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.08 mg/mL (5.84 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.84 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 AICAR phosphate種 AMP 活化蛋激酶 (AMPK) 激活劑，下調(diào) HepG2 細胞中的胰島素受體表達。IC50 & Target AMP

5、K 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. The expression level of IR- significantly decreases with 0.25, 0.5, and 1.0 mM of AICAR at 48h to 50%, 53%, and 46% of the control, respectively 1.體內(nèi)研究 Fourteen-week

6、-old male, lean (L; 31.3 g body wt) wild-type andob/ob (O; 59.6 g body wt) mice are injectedwith the AMP-activated kinase (AMPK) activator AICAR (A) at 0.5 mg*g body wt-1*day-1 or saline control (C)for 14 days. At 24 h after the last injection (including a 12-h fast), all mice are killed, and the pl

7、antar flexorcomplex muscle (gastrocnemius, soleus, and plantaris) is excised for analysis. Muscle mass is lower in OC(15912 mg) than LC, LA, and OA (17610, 1789, and 16616 mg, respectively) mice, independent of abody weight change 2. The kidney weight is significantly higher in the untreated group w

8、hen compared withboth the exercise and AICAR (0.5 mg/g body wt) groups. The heart weight is higher in the exercise groupthan in the other groups, whereas the liver weight is significantly higher in the AICAR-treated group whencompared with the exercise and untreated groups 3.PROTOCOLCell Assay 1 Hep

9、G2 cells (5105 cells) are plated in 6-well culture plate dishes and then are incubated in the serum-freemedia for 12 h before transfection. One microgram of plasmid is transfected with FuGENE6 TransfectionReagent. After 5 h of transfection, the culture media are removed and then media supplemented w

10、ith orwithout AICAR (0.1-1.0 mM) are added to each well. The stimulation media are changed every 24 h 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 2Administration 23 Fourteen-week-old lean (Lepob/+ or Lepob/+) and ob/ob (Lepob/Lepob/) m

11、ale mice are uesd. After the 14-day experimental treatment (24 h after AICAR injection, including a 12-h fast), the plantar flexor complexmuscle is cleanly (tendon-to-tendon) excised from an anesthetized mouse breathing 4% isoflurane. Themuscle is quickly weighed and then processed for histology or

12、frozen in liquid nitrogen and stored at 80C.The anesthetized mice are killed by transection of the diaphragm and removal of the entire heart, after bloodcollection via needle puncture directly into the heart, while breathing 4% isoflurane. AICAR or saline (control)is injected subcutaneously into the

13、 lateral distal portion of the back. AICAR is administered at 0.5 mg*g bodywt-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 that of AICAR treatment. Body weight is measured prior to death.2/3 Master o

14、f Small Molecules 您邊的抑制劑師www.MedChemERats 3Male 5-week-old ZDF rats are either subcutaneously injected with a single dose of AICAR (0.5 mg/g body wt)or underwent a single bout of treadmill running (60 min, speed of 25 m/min at a 5% incline). Untreated ZDFrats serve as controls (n=5 in each group). O

15、ne hour after the subcutaneous AICAR injection or immediatelyafter treadmill running, rats are killed by cervical dislocation. To avoid any effect of muscle spasm andhypoxia, red and white gastrocnemius muscles are removed within seconds and immediately freeze clampedfor later determination of AMPK

16、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 Cell Metab. 2019 Jul 2;30(1):157-173.e7 Oncogene. 2019 Jul 29. Cell Death Dis. 2018 May 1;9(5):515. J Cell Physiol. 2018 Dec;233(12):9701-9715. Biochim Biophys Acta Mol Basis Dis. 2018

17、 Nov;1864(11):3723-3738.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Nakamaru K, et al. AICAR, an activator of AMP-activated protein kinase, down-regulates the insulin receptor expression in HepG2 cells.Biochem Biophys Res Commun. 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 infasted skeletal muscle. Am J Physiol Regul Integr Comp Physiol. 2010 Dec;299(6):R1546-54.3. Pold R, et al. Long-term AICAR administration and e