ESI-09

製品コードS7499 バッチS749903

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 (warmed with 50ºC water bath) 5 mg/mL (15.11 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/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 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, this compound fails to suppress epidermal growth factor (EGF)-induced phosphorylation of Akt in AsPC1 cells. In pancreatic cancer cells, this antagonist inhibits cells migration and invasion through decreasing 007-AM-induced cell adhesion dose-dependently. [1] This chemical significantly reduces intracellular and total bacterial counts in human umbilical vein endothelial cells. [2] It effectively antagonizes Schwann cells (SC) differentiation induced by CPT-cAMP as well as the formation of myelin. In SC-neuron cultures, this compound 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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/23066090/
  • https://pubmed.ncbi.nlm.nih.gov/24218580/
  • https://pubmed.ncbi.nlm.nih.gov/24349260/

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：

Ginsenoside Ro prevents endothelial injury via promoting Epac1/AMPK- mediated mitochondria protection in early diabetic retinopathy [ Pharmacol Res, 2025, 211:107562] PubMed: 39732351
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
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
PNX14 but not PNX20 as a novel regulator of preadipocyte differentiation via activating Epac-ERK signaling pathway in Gallus gallus [ Gen Comp Endocrinol, 2023, 335:114232] PubMed: 36774983
Vitexin Mitigates Myocardial Ischemia/Reperfusion Injury in Rats by Regulating Mitochondrial Dysfunction via Epac1-Rap1 Signaling [ Oxid Med Cell Longev, 2021, 2021:9921982] PubMed: 34257823
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

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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