AdipoRon

製品コードS7365 バッチS736503

印刷

化学情報

Chemical Structure Synonyms SC-396658 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C27H28N2O3
分子量 428.52 CAS No. 924416-43-3
Solubility (25°C)* 体外 DMSO 86 mg/mL (200.69 mM)
Ethanol 86 mg/mL (200.69 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO Corn oil
4.3mg/ml Taking the 1 mL working solution as an example, add 50 μL of 86 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.3mg/ml
* <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 AdipoRon (SC-396658) is a novel, and orally bioavailable adiponectin receptor agonist with KD of 1.8 and 3.1 μM for AdipoR1 and AdipoR2, respectively.
in vitro AdipoRon increases AMPK activation, PGC-1α expression and mitochondrial biogenesis by binding to both AdipoR1 and AdipoR2 in C2C12 myotubes. [1]
in vivo In skeletal muscle and liver of wild-type mice AdipoRon (50 mg/kg, i.v.) significantly induces phosphorylation of AMPK via AdipoR1 and AdipoR2. In WT mice, AdipoRon (50 mg/kg, p.o.) improves insulin resistance, glucose intolerance and dyslipidaemia by activating AdipoR1–AMPK–PGC-1α pathways in skeletal muscle, while by activating AdipoR2–PPAR-α pathways in the liver. Moreover, AdipoRon ameliorates diabetes of genetically obese rodent model db/db mice, and prolongs the shortened lifespan of db/db mice on a high-fat diet. [1]
特徴 Orally bioavailable adiponectin receptor agonist that can be used for the treatment of obesity-related diseases.

プロトコル(参考用のみ)

キナーゼアッセイ Binding assays
Surface plasmon resonance measurements are performed by a BIAcore X100 system and sensor chip SA . Human AdipoR1 and AdipoR2 are expressed with the baculovirus system, and purified to homogeneity. The AdipoR1 and AdipoR2 samples are then reconstituted into egg-phosphatidylcholine liposomes containing biotinyl phosphatidylethanolamine. Mouse full-length adiponectin is generated. AdipoR1 and AdipoR2 are immobilized onto a sensor chip SA to levels of 2,500-3,000 response units (RU) using standard immobilization protocols. Rhodopsin receptor is used as control. Experiments are carried out at 25 ˚C using running buffer (20 mM Hepes, pH 7.4, 200 mM NaCl, 10% glycerol, 0.05% (v/v) surfactant P20). Binding analyses are performed using a range of AdipoRon (0.49-31.25 μM) or adiponectin (1.5 ng-3.75 μg). Biacore X100 Evaluation Software is used to determine the equilibrium dissociation constant (KD) of the compound or proteins.
動物実験 動物モデル The wild-type, Adipor1−/−, Adipor2−/−, Adipor1−/− Adipor2−/− knockout mice and the db/db mice.
投薬量 ~50 mg/kg
投与方法 i.v. or p.o.

カスタマーフィードバック

Data from [Data independently produced by , , Mol Med Rep, 2018, 17(1):209-215]

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：

Small-molecule agonist AdipoRon alleviates diabetic retinopathy through the AdipoR1/AMPK/EGR4 pathway [ J Transl Med, 2024, 22(1):2] PubMed: 38166990
Overexpression of salusin‑β downregulates adipoR1 expression to prevent fatty acid oxidation in HepG2 cells [ Mol Med Rep, 2024, 29(2)18] PubMed: 38063230
Adiponectin suppresses tumor growth of nasopharyngeal carcinoma through activating AMPK signaling pathway [ J Transl Med, 2022, 20(1):89] PubMed: 35164782
Adiponectin Deficiency Promotes Endometrial Carcinoma Pathogenesis and Development via Activation of Mitogen-Activated Protein Kinase [ J Pathol, 2022, 10.1002/path.5874] PubMed: 35072951
SCA-1 micro-heterogeneity in the fate decision of dystrophic fibro/adipogenic progenitors [ Cell Death Dis, 2021, 12(1):122] PubMed: 33495447
Lipophagy deficiency exacerbates ectopic lipid accumulation and tubular cells injury in diabetic nephropathy [ Cell Death Dis, 2021, 12(11):1031] PubMed: 34718329
SCA-1 micro-heterogeneity in the fate decision of dystrophic fibro/adipogenic progenitors [ Cell Death Dis, 2021, 12(1):122] PubMed: 33495447
An adiponectin receptor agonist promote osteogenesis via regulating bone-fat balance [ Cell Prolif, 2021, 54(6):e13035] PubMed: 33939201
AdipoRon Protects against Tubular Injury in Diabetic Nephropathy by Inhibiting Endoplasmic Reticulum Stress [ Oxid Med Cell Longev, 2020, 2020:6104375] PubMed: 32832003
AdipoRon Attenuates Hypertension-Induced Epithelial-Mesenchymal Transition and Renal Fibrosis via Promoting Epithelial Autophagy [ J Cardiovasc Transl Res, 2020, 10.1007/s12265-020-10075-8] PubMed: 33025271

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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