購物車 
-
ESI-09
- names：
ESI-09
- CAS號：
263707-16-0
MDL Number： MFCD00109218 - MF(分子式)： C16H15ClN4O2 MW(分子量)： 330.77
- EINECS:No data available Reaxys Number:No data available
- Pubchem ID:6077765 Brand:BIOFOUNT
ESI-09(263707-16-0)是一種新型非環狀核苷酸EPAC拮抗劑，能夠特異性阻斷細胞內EPAC介導的Rap1活化和Akt磷酸化，以及EPAC介導的胰腺β細胞中胰島分泌。另一方面，ESI-09不抑制AsPC1細胞中表皮生長因子(EGF)誘導的Akt磷酸化。在胰腺癌細胞中，ESI-09通過劑量依賴性降低007-AM誘導的細胞粘附而抑制細胞遷移和侵襲。ESI-09顯著降低人臍靜脈內皮細胞中總細菌數。ESI-09有效拮抗CPT-cAMP誘導的Schwann細胞(SC)分化以及髓鞘的形成。在SC神經元培養基中，ESI-09顯著降低O1陽性和MBP陽性的數量，而不影響神經元或SCs自身的健康。
| 貨品編碼 | 規格 | 純度 | 價格 (￥) | 現價(￥) | 特價(￥) | 庫存描述 | 數量 | 總計 (￥) |
|---|---|---|---|---|---|---|---|---|
| YZM000889-10mg | 10mg | 98% | ￥ 1230.00 | ￥ 1230.00 | 2-3天 | ￥ 0.00 | ||
| YZM000889-5mg | 5mg | 98% | ￥ 698.00 | ￥ 698.00 | 2-3天 | ￥ 0.00 |
| 中文別名 | ESI-09(263707-16-0),ESI09,ESI 09 |
| 英文別名 | ESI-09,263707-16-0,ESI09,ESI 09 |
| CAS號 | 263707-16-0 |
| Inchi | InChI=1S/C16H15ClN4O2/c1-16(2,3)14-8-12(21-23-14)15(22)13(9-18)20-19-11-6-4-5-10(17)7-11/h4-8,19H,1-3H3/b20-13+ |
| InchiKey | DXEATJQGQHDURZ-DEDYPNTBSA-N |
| 分子式 Formula | C16H15ClN4O2 |
| 分子量 Molecular Weight | 330.77 |
| 溶解度Solubility | 生物體外In Vitro:DMSO溶解度≥ 47 mg/mL(142.09 mM)H2O< 0.1 mg/mL(insoluble)*"≥" means soluble可溶, but saturation unknown溶解度未知. |
| 性狀 | 灰白色至橙色固體粉末 |
| 儲藏條件 Storage conditions | 在-20°C條件下保存3年,在4°C條件下保存2年 |
ESI-09(263707-16-0)實驗注意事項：
1.實驗前需戴好防護眼鏡，穿戴防護服和口罩，佩戴手套，避免與皮膚接觸。
2.實驗過程中如遇到有毒或者刺激性物質及有害物質產生，必要時實驗操作需要手套箱內完成以免對實驗人員造成傷害
3.實驗后產生的廢棄物需分類存儲，并交于專業生物廢氣物處理公司處理，以免造成環境污染
ESI-09(263707-16-0)Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.
Tag:ESI-09(263707-16-0),ESI-09抑制劑,ESI-09試劑,ESI-09的作用,ESI-09的純度,ESI-09雜質,ESI-09的外觀,ESI-09的溶解度,ESI-09的用途,ESI-09的合成,ESI-09的生產,ESI-09的注意事項,ESI-09的MSDS
| 產品說明 | ESI-09(263707-16-0)是一種新型非環狀核苷酸EPAC拮抗劑，能夠特異性阻斷細胞內EPAC介導的Rap1活化和Akt磷酸化 |
| Introduction | ESI-09 (263707-16-0) is a new type of non-cyclic nucleotide EPAC antagonist, which can specifically block EPAC-mediated Rap1 activation and Akt phosphorylation in cells |
| Application1 | |
| Application2 | |
| Application3 |
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.ESI-09 is a novel noncyclic 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. EPAC1 plays an important role in pancreatic cancer cell migration and invasion, and thus represents a potential target for developing novel therapeutic strategies for pancreatic cancer.
| 警示圖 | |
| 危險性 | warning |
| 危險性警示 | Not available |
| 安全聲明 | H303吞入可能有害+H313皮膚接觸可能有害+H2413吸入可能對身體有害 |
| 安全防護 | P264處理后徹底清洗+P280戴防護手套/穿防護服/戴防護眼罩/戴防護面具+P305如果進入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續沖洗+P337如果眼睛刺激持續+P2393獲得醫療建議/護理 |
| 備注 | 實驗過程中防止吸入、食入，做好安全防護 |
| Role of Exchange Protein Directly Activated by Cyclic AMP Isoform 1 in Energy Homeostasis: Regulation of Leptin Expression and Secretion in White Adipose Tissue |
| Recent advances in the discovery of small molecules targeting exchange proteins directly activated by cAMP (EPAC) |
| Exchange protein directly activated by cAMP plays a critical role in bacterial invasion during fatal rickettsioses |
| A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion |
| [Differences in the responses of taste receptors to organic and inorganic acids with changes in the concentration of bicarbonate in the solution] |
Epac-inhibitors: facts and artefacts.
Rehmann H1. Sci Rep. 2013 Oct 23;3:3032. doi: 10.1038/srep03032.
cAMP is a universal second messenger. Its signalling is mediated by protein kinase A, Epac and certain types of ion channels in mammalians. cAMP signalling is involved in many physiological processes ranging from vision to the control of insulin secretion, pacemaker activity and gene transcription and therefore selective pharmacological interference is of medical interest. Whereas selective inhibitors of PKA and selective activators of Epac are well established, no inhibitors of Epac were available until recently. Here the action of four of the novel Epac inhibitors was analysed by biophysical means. ESI-05 is confirmed as a selective inhibitor of Epac2. No direct action of Brefeldin A on Epac could be demonstrated. ESI-09 and HJC0197 were found to act as chemicals with general protein denaturing properties and do not act on Epac selectively.
Rehmann H1. Sci Rep. 2013 Oct 23;3:3032. doi: 10.1038/srep03032.
cAMP is a universal second messenger. Its signalling is mediated by protein kinase A, Epac and certain types of ion channels in mammalians. cAMP signalling is involved in many physiological processes ranging from vision to the control of insulin secretion, pacemaker activity and gene transcription and therefore selective pharmacological interference is of medical interest. Whereas selective inhibitors of PKA and selective activators of Epac are well established, no inhibitors of Epac were available until recently. Here the action of four of the novel Epac inhibitors was analysed by biophysical means. ESI-05 is confirmed as a selective inhibitor of Epac2. No direct action of Brefeldin A on Epac could be demonstrated. ESI-09 and HJC0197 were found to act as chemicals with general protein denaturing properties and do not act on Epac selectively.
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