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HomeProduct name listA 205804

A 205804

A 205804 Structural

What is A 205804?

Description

A-205804 is a potent inhibitor of E-selectin and ICAM-1 expression in human vascular endothelial cells stimulated with TNF-α (IC50s = 20 and 25 nM, respectively). It does not block expression of VCAM-1 (IC50 > 1,000 nM).

The Uses of A 205804

4-[(4-Methylphenyl)thio]thieno[2,3-c]pyridine-2-carboxamide is a reagent used in the preparation of selective inhibitors of cell adhesion molecule expression in human endothelial cells.

What are the applications of Application

A 205804 is a selective inhibitor of E-selectin and ICAM-1 expression

Definition

ChEBI: 4-[(4-methylphenyl)thio]-2-thieno[2,3-c]pyridinecarboxamide is an aryl sulfide.

Biological Activity

Selective inhibitor of E-selectin and ICAM-1 expression (IC 50 values are 20, 25 and > 1000 nM for TNF- α -induced E-selectin, ICAM-1 and VCAM-1 expression respectively). Effective inhibitor of cell-cell adhesion in an in vitro flow experiment.

storage

Store at +4°C

References

[1]. stewart, a.o., et al., discovery of inhibitors of cell adhesion molecule expression in human endothelial cells. 1. selective inhibition of icam-1 and e-selectin expression. j med chem, 2001. 44(6): p. 988-1002.
[2]. chang, c.z., et al., valproic acid attenuates intercellular adhesion molecule-1 and e-selectin through a chemokine ligand 5 dependent mechanism and subarachnoid hemorrhage induced vasospasm in a rat model. j inflamm (lond), 2015. 12: p. 27.
[3]. zhu, g.d., et al., selective inhibition of icam-1 and e-selectin expression in human endothelial cells. 2. aryl modifications of 4-(aryloxy)thieno[2,3-c]pyridines with fine-tuning at c-2 carbamides. j med chem, 2001. 44(21): p. 3469-87.
[4]. zhu, g.d., et al., synthesis and mode of action of (125)i- and (3)h-labeled thieno[2,3-c]pyridine antagonists of cell adhesion molecule expression. j org chem, 2002. 67(3): p. 943-8.

Properties of A 205804

Melting point: 198-199℃
Boiling point: 581.3±45.0 °C(Predicted)
Density  1.40±0.1 g/cm3(Predicted)
storage temp.  Sealed in dry,2-8°C
solubility  ≥30 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
pka 15.12±0.30(Predicted)
form  powder to crystal
color  White to Orange to Green

Safety information for A 205804

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for A 205804

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