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ESI-09
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ESI-09图片
CAS NO:263707-16-0
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)330.77
FormulaC16H15ClN4O2
CAS No.263707-16-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 66 mg/mL (199.5 mM)
Water: <1 mg/mL
Ethanol: 20 mg/mL (60.5 mM)
Other info

Chemical Name: (E)-2-(5-(tert-butyl)isoxazol-3-yl)-N'-(3-chlorophenyl)-2-oxoacetohydrazonoyl cyanide

InChi Key: DXEATJQGQHDURZ-DEDYPNTBSA-N

InChi Code: 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+

SMILES Code: N#C/C(C(C1=NOC(C(C)(C)C)=C1)=O)=N\NC2=CC=CC(Cl)=C2

Synonyms

ESI-09; ESI 09; ESI09

实验参考方法
In Vitro

In vitro activity: 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. ESI-09 significantly reduces intracellular and total bacterial counts in human umbilical vein endothelial cells. 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.


Cell Assay: In the pancreatic cancer cell line AsPC-1, ESI-09 inhibited Akt phosphorylation at T308 and S473 stimulated by 007-AM in a dose dependent way. In pancreatic endocrine β cells, ESI-09 inhibited the increase of insulin secretion stimulated by 007-AM in a dose dependent way. In pancreatic cancer cell lines AsPC-1 and PANC-1, ESI-09 significantly reduced cell migration through the inhibition of EPAC1.

In VivoESI-09 (10 mg/kg/d, i.p.), via pharmacological inhibition of EPAC1, protects WT C57BL/6 mice from fatal SFG rickettsiosis.
Animal modelEpac1+/+ mice
Formulation & DosageDissolved in buffer saline containing 10% ethanol and 10% Tween-80; 10 mg/kg/d; i.p. injection
References

Mol Pharmacol. 2013 Jan;83(1):122-8; Proc Natl Acad Sci U S A. 2013 Nov 26;110(48):19615-20; PLoS One. 2013 Dec 11;8(12):e82354.