ESI-09

製品コードS7499 バッチS749902

印刷

化学情報

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

C16H15ClN4O2
分子量 330.77 CAS No. 263707-16-0
Solubility (25°C)* 体外 DMSO 66 mg/mL (199.53 mM)
Ethanol 17 mg/mL warmed with 50ºC water bath (51.39 mM)
Water Insoluble
* <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 ESI-09 is a specific exchange protein directly activated by cAMP (EPAC) inhibitor with IC50 of 3.2 μM and 1.4 μM for EPAC1 and EPAC2, respectively, >100-fold selectivity over PKA.
in vitro ESI-09, a novel non-cyclic nucleotide EPAC antagonist, that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic β cells. On the other hand, ESI-09 fails to suppress epidermal growth factor (EGF)-induced phosphorylation of Akt in AsPC1 cells. In pancreatic cancer cells, ESI-09 inhibits cells migration and invasion through decreasing 007-AM-induced cell adhesion dose-dependently. [1] ESI-09 significantly reduces intracellular and total bacterial counts in human umbilical vein endothelial cells. [2] ESI-09 effectively antagonizes Schwann cells (SC) differentiation induced by CPT-cAMP as well as the formation of myelin. In SC-neuron cultures, ESI-09 dramatically reduces the number of O1 positive and MBP positive SCs without compromising the health of the neurons or the SCs themselves. [3]
in vivo ESI-09 (10 mg/kg/d, i.p.), via pharmacological inhibition of EPAC1, protects WT C57BL/6 mice from fatal SFG rickettsiosis. [2]

プロトコル(参考用のみ)

キナーゼアッセイ EPAC activity assays
In brief, Purified samples containing GTP-bound Rap1 are denatured in SDS loading buffer, resolved by 15% denaturing polyacrylamide gel electrophoresis (SDS-PAGE) and analyzed by western blotting using anti-Rap1 antibodies. Samples from total cell lysates are also analyzed as controls for total Rap1 expression.
動物実験 動物モデル Epac1+/+ mice
投薬量 10 mg/kg/d
投与方法 i.p.

カスタマーフィードバック

, , Brain Behav Immun, 2016, 58:118-129.

Data from [Data independently produced by , , Biomed Pharmacother, 2019, 109:1268-1275]

Data from [Data independently produced by , , Acta Diabetol, 2017, 54(6):581-591]

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：

Inhibition of exchange proteins directly activated by cAMP as a strategy for broad-spectrum antiviral development [ J Biol Chem, 2023, 299(6):104749] PubMed: 37100284
Terbutaline attenuates LPS-induced injury of pulmonary microvascular endothelial cells by cAMP/Epac signaling [ Drug Dev Res, 2021, 10.1002/ddr.21901] PubMed: 34846077
Knockdown of GPSM1 Inhibits the Proliferation and Promotes the Apoptosis of B-Cell Acute Lymphoblastic Leukemia Cells by Suppressing the ADCY6-RAPGEF3-JNK Signaling Pathway [ Pathol Oncol Res, 2021, 27:643376] PubMed: 34257610
Exchange protein directly activated by cAMP (Epac) 1 plays an essential role in stress-induced exercise capacity by regulating PGC-1α and fatty acid metabolism in skeletal muscle. [ Pflugers Arch, 2020, 472(2):195-216] PubMed: 31955265
Curcumin pretreatment protects against hypoxia/reoxgenation injury via improvement of mitochondrial function, destabilization of HIF-1α and activation of Epac1-Akt pathway in rat bone marrow mesenchymal stem cells [Wang X, et al. Biomed Pharmacother, 2019, 109:1268-1275] PubMed: 30551377
Protective Effect of Quercetin in LPS-Induced Murine Acute Lung Injury Mediated by cAMP-Epac Pathway [Wang XF, et al. Inflammation, 2018, 41(3):1093-1103] PubMed: 29569077
Activation of Epac alleviates inflammation and vascular leakage in LPS-induced acute murine lung injury [Wang X, et al. Biomed Pharmacother, 2017, 96:1127-1136] PubMed: 29174852
The microRNA-7-mediated reduction in EPAC-1 contributes to vascular endothelial permeability and eNOS uncoupling in murine experimental retinopathy. [Garcia-Morales V, et al. Acta Diabetol, 2017, 54(6):581-591] PubMed: 28353063
Bile Acids Control Inflammation and Metabolic Disorder through Inhibition of NLRP3 Inflammasome [Guo C, et al. Immunity, 2016, 45(4):944] PubMed: 27760343
Cannabinoid receptor-2 stimulation suppresses neuroinflammation by regulating microglial M1/M2 polarization through the cAMP/PKA pathway in an experimental GMH rat model [Tao Y, et al. Brain Behav Immun, 2016, 10.1016/j.bbi.2016.05.020] PubMed: 27261088

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。