Home PI3K/Akt/mTOR AMPK 활성제 AICAR (Acadesine)

연구용

AICAR (Acadesine) AMPK 활성제

제품 번호: S1802

AICAR (Acadesine, NSC105823, AICA Riboside)은 AMPK 활성제로, AMPK 및 AMPK kinase에 대한 AMP의 자극 효과를 모방하는 ZMP의 축적을 유발합니다. 이 화합물은 Mitophagy를 유도합니다. 임상 3상.
AICAR (Acadesine) AMPK 활성제 Chemical Structure

화학 구조

분자량: 258.23

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품질 관리 (Quality Control)

배치: 순도: 99.97%
99.97

함께 자주 사용되는 제품 AICAR (Acadesine)

Tanespimycin (17-AAG)

Treatment with this compound and 17-AAG reduces cell proliferation and affects chromosome segregation in MEFs and human cancer cells.

Nutlin-3a

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

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
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
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
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 Inhibition of adipogenesis in mouse 3T3L1 cells assessed as reduction in triglyceride content at 0.2 mM by colorimetric assay 26088335
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
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 258.23 화학식

C9H14N4O5

 보관 (수령일로부터)
CAS 번호 2627-69-2 SDF 다운로드 원액 보관

동의어 NSC105823, AICA Riboside Smiles C1=NC(=C(N1C2C(C(C(O2)CO)O)O)N)C(=O)N

용해도 (Solubility)

In vitro
배치:

DMSO : 51 mg/mL (197.49 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 20 mg/mL

Ethanol : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

특징
A potential first-in-class ARA.
Targets/IC50/Ki
AMPK
(Cell-free assay)
AMPKK
(Cell-free assay)
시험관 내(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. This compound 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. It also causes a dramatic inhibition of both fatty acid and sterol synthesis in rat hepatocytes, as well as a dramatic inactivation of HMG-CoA reductase. AICAR induces apoptosis of B-CLL cells in a dose-dependent manner with EC50 of 380 μM. At 0.5 mM, it decreases cell viability of B-CLL cells from 20 representative patients from 68% to 26%, and induces caspase activation and cytochrome c release from mitochondria. Uptake and phosphorylation of the compound are required to induce apoptosis and activate AMPK in B-CLL cells. While concentrations of 2-4 mM only slightly affect the viability of T cells from B-CLL patients, 0.5 mM remarkedly reduces viability of B cells but not T cells. It 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 AICAR is abrogated by GF109203X and Ro-32-0432, both inhibitor of classical and new PKCs and accordingly, it triggers relocation and activation of several PKC isoforms in K562 cells. The compound dose-dependently inhibits K562 colony formation at day 10, the growth inhibitory effect is already detected at 0.25 mM and is maximal at 2.5 mM. AICAR causes a concentration-related reduction in CD18 expression on LPS-stimulated neutrophils in vitro. It significantly (1 mM) inhibits N-formyl-methionyl-leucyl-phenylalanine-induced granulocyte CD11b up-regulation by a mean of 61% in blood.

생체 내(In vivo)

Acadesine (50 mg/kg) significantly reduces tumor formation in a mouse xenograft model of K562 cells. At 10 mg/kg, this compound results in higher fluid required to stabilize hemodynamics in pigs and inhibits LPS-induced protein permeability of pulmonary capillaries, peak inspiratory pressures on constant tidal volume and dead space ventilation.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/8619186/
  • [5] https://pubmed.ncbi.nlm.nih.gov/7877305/

적용 분야 (Applications)

방법 바이오마커 이미지 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
S1802-WB1
26528831
Immunofluorescence p-ERK YAZ / TAZ
S1802-IF1
26528831