A 205804
- CAS NO.:251992-66-2
- Empirical Formula: C15H12N2OS2
- Molecular Weight: 300.4
- MDL number: MFCD09038566
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-07 13:31:19
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) |
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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