A-205804

Catalog No.S2885

A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 expression with IC50 of 20 nM and 25 nM respectively.

Price Stock Quantity  
USD 140 In stock
USD 110 In stock
USD 470 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

A-205804 Chemical Structure

A-205804 Chemical Structure
Molecular Weight: 300.4

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

A-205804 is available in the following compound libraries:

Product Information

  • Compare Integrin Inhibitors
    Compare Integrin Products
  • Research Area

Product Description

Biological Activity

Description A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 expression with IC50 of 20 nM and 25 nM respectively.
Targets E-selectin [1] ICAM-1 [1]
IC50 20 nM 25 nM
In vitro 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. [2]
In vivo
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Cell ELISA Assay Primary HUVECs are plated in 96-well plates at 5 × 104 cells/mL in EBM/2% FBS/human epidermal growth factor/bovine brain extract/gentamicin. The following day test compounds are added and the plates incubats for 24 h at 37 °C. TNFα then is added to a final concentration of 5 ng/mL, and the plates are incubated for an additional 6 h at 37 °C. The plates are washed once with D-PBS, and primary antibody is added in D-PBS/2% BSA /0.01% NaN3. The antibodies used are mouse monoclonal anti-ELAM-1, anti-ICAM-1, and anti-VCAM-1. The plates are stored overnight at 4 °C and then washes three times with D-PBS. Secondary antibody, HRP-conjugated donkey anti-mouse IgG in D-PBS/2%BSA, is added, and the plates are incubated for 1−2 h at room temperature and then washes three times with D-PBS. OPD solution is added to the wells, the plates are developed for 15−20 min and neutralizes with 1 N sulfuric acid, and the absorbance is read at 490 nm.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Zhu GD, et al. J Med Chem, 2001, 44(21), 3469-3487.

[2] Stewart AO, J Med Chem, 2001, 44(6), 988-1002.

Chemical Information

Download A-205804 SDF
Molecular Weight (MW) 300.4
Formula

C15H12N2OS2

CAS No. 251992-66-2
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 60 mg/mL (199.73 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Thieno[2,3-c]pyridine-2-carboxamide, 4-[(4-methylphenyl)thio]-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related Integrin Products

Recently Viewed Items

Tags: buy A-205804 | A-205804 supplier | purchase A-205804 | A-205804 cost | A-205804 manufacturer | order A-205804 | A-205804 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us