A-205804
Based on 5 publication(s) in Google Scholar
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 98.96%
- CAS No.: 251992-66-2
- 화학식: C15H12N2OS2
- 분자량:300.40
-
보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
용액&용해도
- 순도&문서
- References
-
Help & FAQs
-
Cytoskeleton Compound Library
HY-L060
-
Orally Active Compound Library
HY-L061
-
Heterocyclic Compound Library
HY-L138
-
Membrane Protein-targeted Compound Library
HY-L149
-
Highly Selective Inhibitors Library
HY-L158
-
Extracellular Vesicles (EVs) Compound Library
HY-L168
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
MCE Kinase Hinge Binder Fragment Library
HY-L907
-
Immunology/Inflammation Compound Library
HY-L007
Publications Citing Use of MedChemExpress (MCE) A-205804
More
Customer Validation & Images
-
RT-PCR
-
WB
-
IF
-
Cell Migration/Invasion Assay
Biological Activity
IC50: 20 nM (E-selectin), 25 nM (ICAM-1)[1]
|
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] |
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 (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
Chemical Information
-
CAS No. 251992-66-2
-
Appearance Solid
-
분자량 300.40
-
화학식 C15H12N2OS2
-
Color Off-white to light yellow
-
SMILES
O=C(C(S1)=CC2=C1C=NC=C2SC3=CC=C(C)C=C3)N
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
-
Journal Impact Factor
-
Most Recent
-
Sci Adv
Earlier onset of chemotherapy-induced neuropathic pain in females by ICAM-1-mediated accumulation of perivascular macrophages. [Abstract]2025 Apr 18;11(16):eadu2159. PMID: 40238872 -
J Immunother Cancer
Targeting TBK1 potentiates oncolytic virotherapy via amplifying ICAM1-mediated NK cell immunity in chemo-resistant colorectal cancer. [Abstract]2025 Jun 8;13(6):e011455. PMID: 40484646 -
Cell Commun Signal
2025 Aug 26;23(1):381. PMID: 40859363
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.
-
Am J Respir Cell Mol Biol
GP IIb/IIIa-ICAM-1 Mediated Platelet-Endothelial Adhesion Exacerbates Pulmonary Hypertension. [Abstract]2025 Feb 28. PMID: 40019848 -
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
-
Data Sheet (276 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
[1]. Stewart AO, 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 Mar 15;44(6):988-1002. [Content Brief]
[2]. Morita K, et al. RUNX transcription factors potentially control E-selectin expression in the bone marrow vascular niche in mice. Blood Adv. 2018 Mar 13;2(5):509-515. [Content Brief]
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 |
A-205804 Related Classifications
HY-100226 Related Classifications
Powered by Bioz