AICAR
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AICAR ??
- ???
- 214-215 °C
- ?? ?
- 726.3±60.0 °C(Predicted)
- ??
- 2.06±0.1 g/cm3(Predicted)
- ?? ??
- -20°C
- ???
- H2O: >10 mg/mL
- ??? ??
- ??
- ?? ?? (pKa)
- 13.27±0.70(Predicted)
- ??
- ??? ? ???
- ???? ??
- rabbit
- ???
- 2mg/ml? DMSO? ?????. 1mg/ml ???? ??? ???? ?????.
- ?? ??(λmax)
- 265nm(NaOH)(lit.)
- Merck
- 14,16
- Specific Activity
- 255-345nmol/min·mg
- ???
- ??? ?? ?????? 2? ?? ??????. DMSO ?? ???? ??? ??? -20°C?? ?? 3?? ?? ??? ? ????.
- InChIKey
- RTRQQBHATOEIAF-UUOKFMHZSA-N
- CAS ??????
- 2627-69-2(CAS DataBase Reference)
??
- ?? ? ?? ??
- ?? ? ???? ?? (GHS)
| ??? ?? | Xi,T | ||
|---|---|---|---|
| ?? ???? ?? | 36/37/38-61 | ||
| ????? | 26-36-45-53 | ||
| WGK ?? | 3 | ||
| TSCA | Yes | ||
| HS ?? | 29349990 |
| ????(GHS): |
 
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| ?? ?: | Danger | |||||||||||||||||||||
| ??·?? ??: |
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AICAR C??? ??, ??, ??
??? ??
Solid??
AICAR is a nucleoside analogue that is able to enter nucleoside pools and is able to significantly increase levels of adenosine during periods of ATP breakdown. Adenosine-regulating agents (ARAs) hav e been recognized for therapeutic potential in myocardial ischemia. Cardioprotective.??
ChEBI: A 1-ribosylimidazolecarboxamide in which the carboxamide group is situated at position 4 of the imidazole ring, which is further substituted at position 5 by an amino group. A purine nucleoside analogue and activator of AMP-activated protein kinase, it is is used for the treatment of acute lymphoblastic leukemia and is reported to have cardioprotective effects.?? ??
Adenosine monophosphate?protein kinase (AMPK) activator 5-aminoimidazole-4-carboxamide?ribonucleotide?(AICAR)?modulates cellular energy. It regulates lipid and glucose metabolism, pro-inflammatory responses,?cytokine production,?cell proliferation and apoptosis. AICAR improves ischemia or reperfusion injury and kidney fibrosis in rats. It provides protection against acute tubular necrosis.???? ??
Cell-permeable, allosteric activator of AMP-activated protein kinase (AMPK). Augments proliferation, differentiation and mineralization of osteoblastic MC3T3-EI cells and attenuates psychosine-induced expression of proinflammatory cytokines and iNOS in astrocytes.???
AICAR is an AMPK (adenosine 5′-monophosphate (AMP)-activated protein kinase) activator that has been shown to have significant endurance-enhancing effects and is banned for use as a doping agent by the World Anti-Doping Agency. Overactivation of AMPK, or activation in the wrong tissues, can lead to serious side effects, including neurodegeneration or preventing cell division. Accumulation of naturally occurring AICAR in the body has also been linked to metabolic disorders in humans. However, AICAR has not been approved for human treatment and cannot be used as a drug. Therefore, its safety has yet to be verified.Clinical claims and research
AICAR has proved in vivo anti-tumor effects in xenograft models. It is currently under clinical trial phase I/II to treat patients with chronic lymphocytic leukemia and has shown good safety and tolerability properties, although some side effects have been reported.AICAR ?? ?? ? ???
???
?? ??
AICAR ?? ??
???( 363)?? ??
| ??? | ?? | ??? | ?? | ?? ? | ?? |
|---|---|---|---|---|---|
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AICAR ?? ??:
???? 5′-????????
AICAR (phosphate)
Inosine Impurity 1
L-Inosine
Inosine
2-CHLOROINOSINE
IDP
XANTHOSINE
2',3',5'-TRI-O-ACETYLINOSINE
GUANOSINE 3':5'-CYCLIC MONOPHOSPHATE SODIUM SALT
2',3'-O-Isopropylideneinosine
XANTHOSINE 5'-MONOPHOSPHATE DISODIUM SALT
3'-GMP DISODIUM SALT
2'-Deoxyguanosine-5'-diphosphate trisodium salt
Succino-AICAR
5-Amino-4-imidazolecarboxamide
CYTIDYLYL-(3'->5')-GUANOSINE