Art. -Nr.: HY-120628

BMS-587101

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BMS-587101 is a potent and orally active antagonist of leukocyte function associated antigen-1 (LFA-1). BMS-587101 has anti-inflammatory effects and can be used for rheumatoid arthritis research.

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Reinheit: 99.39%
CAS. Nr.: 509083-77-6
Formel: C₂₆H₂₀Cl₂N₄O₄S
Molecular Weight:555.43

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

BMS-587101 Chemical Structure

CAS. Nr.: 509083-77-6

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

BMS-587101 is a potent and orally active antagonist of leukocyte function associated antigen-1 (LFA-1). BMS-587101 has anti-inflammatory effects and can be used for rheumatoid arthritis research^[1]^[2].

Alle Integrin Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
bEND	IC₅₀	150 nM Compound: 8, BMS-587101	Inhibition of mouse bEND cell adhesion to T cell Inhibition of mouse bEND cell adhesion to T cell	[PMID: 17125246]
HUVEC	IC₅₀	18 nM Compound: 1, BMS-688521	Inhibition of LFA1-mediated adhesion of human T cells to ICAM1-expressing HUVEC by fluorescence assay Inhibition of LFA1-mediated adhesion of human T cells to ICAM1-expressing HUVEC by fluorescence assay	[PMID: 20405922]
HUVEC	IC₅₀	20 nM Compound: 8, BMS-587101	Inhibition of LFA1-mediated adhesion of T cell to HUVEC Inhibition of LFA1-mediated adhesion of T cell to HUVEC	[PMID: 17125246]
PBMC	IC₅₀	280 nM Compound: 8, BMS-587101	Antiproliferative activity against PBMC by MLR assay Antiproliferative activity against PBMC by MLR assay	[PMID: 17125246]
T-cell	IC₅₀	150 nM Compound: 1, BMS-688521	Inhibition of LFA1-mediated adhesion of C57BL/6 mouse T cells to ICAM1-expressing TNF-alpha-activated mouse b.END3 cells by calcein-AM staining-based fluorescence assay Inhibition of LFA1-mediated adhesion of C57BL/6 mouse T cells to ICAM1-expressing TNF-alpha-activated mouse b.END3 cells by calcein-AM staining-based fluorescence assay	[PMID: 20405922]
T-cell	IC₅₀	280 nM Compound: 1, BMS-688521	Inhibition of LFA1-mediated human T cell proliferation assessed as [3H]thymidine uptake after 4 days by mixed lymphocyte reaction assay Inhibition of LFA1-mediated human T cell proliferation assessed as [3H]thymidine uptake after 4 days by mixed lymphocyte reaction assay	[PMID: 20405922]

In Vitro

BMS-587101 is a moderately potent inhibitor of LFA-1-mediated T-cell proliferation, with an IC₅₀ of 20 nM in human HUVEC cells. BMS-587101 inhibits LFA-1-mediated adhesion of T cells to endothelial cells, T cell proliferation, and Th1 cytokine production^[1]^[2].
? In mouse splenocytes and a mouse ICAM-1 expressing cell lines, bEND, BMS-587101 shows inhibitory activities, with an IC₅₀ of 150 nM^[1].

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

In Vivo

In the mouse ovalbumin-induced lung inflammation model, BMS-587101 (0.1 mg/kg, 1.0 mg/kg, and 10 mg/kg; po.; twice a day) treatment significantly inhibits eosinophil accumulation^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 509083-77-6
Appearance Solid
Molecular Weight 555.43
Formel C₂₆H₂₀Cl₂N₄O₄S
Color Off-white to light yellow
SMILES

O=C(C1=CSC(CN(C[C@H]2C3=CC=C(C#N)C=C3)C[C@]2(N(C)C(N4C5=CC(Cl)=CC(Cl)=C5)=O)C4=O)=C1)O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 260 mg/mL (468.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8004 mL

9.0020 mL

18.0041 mL

5 mM

0.3601 mL

1.8004 mL

3.6008 mL

10 mM

0.1800 mL

0.9002 mL

1.8004 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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% Corn Oil

Solubility: ≥ 6.5 mg/mL (11.70 mM); Clear solution

This protocol yields a clear solution of ≥ 6.5 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 (65.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Dominique Potin, et al. Discovery and development of 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl-methyl]-3-thiophenecarboxylic acid (BMS-587101)--a small molecule antagonist of leukocyte function a [Content Brief]

[2]. Suzanne J Suchard, et al. An LFA-1 (alphaLbeta2) small-molecule antagonist reduces inflammation and joint destruction in murine models of arthritis. J Immunol. 2010 Apr 1;184(7):3917-26. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8004 mL	9.0020 mL	18.0041 mL	45.0102 mL
	5 mM	0.3601 mL	1.8004 mL	3.6008 mL	9.0020 mL
	10 mM	0.1800 mL	0.9002 mL	1.8004 mL	4.5010 mL
	15 mM	0.1200 mL	0.6001 mL	1.2003 mL	3.0007 mL
	20 mM	0.0900 mL	0.4501 mL	0.9002 mL	2.2505 mL
	25 mM	0.0720 mL	0.3601 mL	0.7202 mL	1.8004 mL
	30 mM	0.0600 mL	0.3001 mL	0.6001 mL	1.5003 mL
	40 mM	0.0450 mL	0.2251 mL	0.4501 mL	1.1253 mL
	50 mM	0.0360 mL	0.1800 mL	0.3601 mL	0.9002 mL
	60 mM	0.0300 mL	0.1500 mL	0.3001 mL	0.7502 mL
	80 mM	0.0225 mL	0.1125 mL	0.2251 mL	0.5626 mL
	100 mM	0.0180 mL	0.0900 mL	0.1800 mL	0.4501 mL

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BMS-587101

Immunology/Inflammation Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Cytoskeleton Compound Library

Orally Active Compound Library

Protein-protein Interaction Inhibitor Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Extracellular Vesicles (EVs) Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Alle Integrin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BMS-587101

Immunology/Inflammation Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Cytoskeleton Compound Library

Orally Active Compound Library

Protein-protein Interaction Inhibitor Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Extracellular Vesicles (EVs) Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Alle Integrin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BMS-587101 Related Classifications

HY-120628 Related Classifications