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A-205804 

Cat. No.: HY-100226 Purity: 98.10%
Handling Instructions

A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC50 of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases.

For research use only. We do not sell to patients.

A-205804 Chemical Structure

A-205804 Chemical Structure

CAS No. : 251992-66-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 121 In-stock
Estimated Time of Arrival: December 31
10 mg USD 110 In-stock
Estimated Time of Arrival: December 31
50 mg USD 440 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC50 of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases[1].

IC50 & Target

IC50: 20 nM (E-selectin), 25 nM (ICAM-1)[1]

In Vitro

A-205804 exhibits Cellular Toxicities for HUVEC with an IC50 of 152 μM[1].
A-205804 is an effective inhibitor of cell-cell adhesion in an in vitro flow experiment, demonstrating relevance in a model physiological system[1].

In Vivo

A-205804 (5 mg/kg; p.o.) shows a half-life of 1 hour for rat[1].
A-205804 (10 mg/kg; p.o.; 3 times per week; for 2 weeks) attenuates the E-selectin expression on the endothelial vascular niche cells in mice[2].

Animal Model: C57BL/6 mice[2]
Dosage: 10 mg/kg
Administration: Oral administration, 3 times per week, for 2 weeks
Result: Efficiently decreased the expression of E-selectin on the endothelial vascular niche cells
Animal Model: Rat[1]
Dosage: 5 mg/kg (Pharmacokinetic Analysis)
Administration: Oral administration
Result: t1/2 = 1 hour
Molecular Weight

300.40

Formula

C₁₅H₁₂N₂OS₂

CAS No.

251992-66-2

SMILES

O=C(C(S1)=CC2=C1C=NC=C2SC3=CC=C(C)C=C3)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (416.11 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3289 mL 16.6445 mL 33.2889 mL
5 mM 0.6658 mL 3.3289 mL 6.6578 mL
10 mM 0.3329 mL 1.6644 mL 3.3289 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (6.92 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.92 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.10%

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Keywords:

A-205804A205804A 205804IntegrinAdhesionmoleculesE-selectinICAM-1Inhibitorinhibitorinhibit

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Product Name:
A-205804
Cat. No.:
HY-100226
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