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A-205804
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。
A-205804图片
CAS NO:251992-66-2
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)300.4
FormulaC15H12N2OS2
CAS No.251992-66-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 60 mg/mL (199.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other info

Chemical Name: 4-[(4-Methylphenyl)thio]thieno[2,3-c]pyridine-2-carboxamide

InChi Key: QQGWEXFLMJGCAL-UHFFFAOYSA-N

InChi Code: 1S/C15H12N2OS2/c1-9-2-4-10(5-3-9)19-13-7-17-8-14-11(13)6-12(20-14)15(16)18/h2-8H,1H3,(H2,16,18)

SMILES Code: CC1=CC=C(SC2=C3C=C(SC3=CN=C2)C(N)=O)C=C1

Synonyms

A205804; A-205804; A 205804

实验参考方法
In Vitro

In vitro activity: A-205804 selectively inhibits the surface expression of the cell adhesion molecules ICAM-1 and E-selectin in human endothelial cells. A-205804 inhibites the IL-1β-induced expression of E-selectin (IC50 = 20 nM) and ICAM-1 (IC50 = 10 nM) with essentially the same level of potency as that for TNFα-induced expression. For reasons which are unclear, the ability of A-205804 to inhibit PMA-induced E-selectin expression is significantly reduced (IC50> 1000 nM), but A-205804 is a potent inhibitor of ICAM-1 expression (IC50 = 40 nM) using this protein-kinase C-activating agent.


Cell Assay: In human vascular endothelial cells using whole-cell high-throughput assay, it was shown that A-205804 exhibited potent and selective inhibition to E-selectin and ICAM-1 with low concentrations. Further, it was revealed that A-205804 inhibited E-selectin and ICAM-1 expressions by translocating to cell nucleus and noncovalently associated with macromolecules of molecular weight greater than 650 kDa when tested with human umbilical vein endothelial cells (HUVECs).

In Vivo
Animal model
Formulation & Dosage
References

J Med Chem. 2001 Oct 11;44(21):3469-87; J Med Chem. 2001 Mar 15;44(6):988-1002.