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  4. A-205804

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.

CAS No. : 251992-66-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 5 publication(s) in Google Scholar

A-205804 Related Antibodies

Top Publications Citing Use of Products

    A-205804 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Aug 26;23(1):381.  [Abstract]

    Confluent HUVECs were treated with A205804 (10 nM, 100 nM, or 1 mM) in the presence of 10 µg/mL Calreticulin for 24 h, and ICAM-1 expression levels were determined by RT-qPCR.

    A-205804 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Aug 26;23(1):381.  [Abstract]

    Confluent HUVECs were treated with A205804 (10 nM, 100 nM, or 1 mM) in the presence of 10 µg/mL Calreticulin for 24 h, and ICAM-1 expression levels were determined by d western blotting.

    A-205804 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Aug 26;23(1):381.  [Abstract]

    Confluent HUVECs were treated with A205804 (10 nM, 100 nM, or 1 mM) in the presence of 10 µg/mL Calreticulin for 24 h of neutrophils to endothelial cells were evaluated.

    A-205804 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Aug 26;23(1):381.  [Abstract]

    HUVECs were treated with 1mM A205804 and 10 µg/mL Calreticulin for 24 h, after which the transendothelial migration.

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    αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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]
    Cellular Effect
    Cell Line Type Value Description References
    HUVEC IC50
    152 μM
    Compound: 1
    Toxicity in HUVEC cell lysates
    Toxicity in HUVEC cell lysates
    		[PMID: 11585452]
    HUVEC IC50
    152 μM
    Compound: 7
    In vitro cellular toxicity against human umbilical vein endothelial cells (HUVEC) in MTS assay
    In vitro cellular toxicity against human umbilical vein endothelial cells (HUVEC) in MTS assay
    		[PMID: 11300880]
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    A-205804 Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    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.
    Appearance

    Solid

    Color

    Off-white to light yellow

    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 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (332.89 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 98.96%

    SDS (393 KB)

    COA (250 KB) HNMR (140 KB) RP-HPLC (204 KB) LCMS (234 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.3289 mL 16.6445 mL 33.2889 mL 83.2224 mL
    5 mM 0.6658 mL 3.3289 mL 6.6578 mL 16.6445 mL
    10 mM 0.3329 mL 1.6644 mL 3.3289 mL 8.3222 mL
    15 mM 0.2219 mL 1.1096 mL 2.2193 mL 5.5482 mL
    20 mM 0.1664 mL 0.8322 mL 1.6644 mL 4.1611 mL
    25 mM 0.1332 mL 0.6658 mL 1.3316 mL 3.3289 mL
    30 mM 0.1110 mL 0.5548 mL 1.1096 mL 2.7741 mL
    40 mM 0.0832 mL 0.4161 mL 0.8322 mL 2.0806 mL
    50 mM 0.0666 mL 0.3329 mL 0.6658 mL 1.6644 mL
    60 mM 0.0555 mL 0.2774 mL 0.5548 mL 1.3870 mL
    80 mM 0.0416 mL 0.2081 mL 0.4161 mL 1.0403 mL
    100 mM 0.0333 mL 0.1664 mL 0.3329 mL 0.8322 mL
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    A-205804 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    A-205804251992-66-2A205804A 205804IntegrinAdhesionmoleculesE-selectinICAM-1Inhibitorinhibitorinhibit

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