Description
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.
Product information
CAS Number: 509083-77-6
Molecular Weight: 555.43
Formula: C26H20Cl2N4O4S
Chemical Name: 5-{[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl]methyl}thiophene-3-carboxylic acid
Smiles: CN1C(=O)N(C2C=C(Cl)C=C(Cl)C=2)C(=O)[C@@]21CN(C[C@H]2C1C=CC(=CC=1)C#N)CC1=CC(=CS1)C(O)=O
InChiKey: NXNKJLOEGWSJGI-BKMJKUGQSA-N
InChi: InChI=1S/C26H20Cl2N4O4S/c1-30-25(36)32(20-8-18(27)7-19(28)9-20)24(35)26(30)14-31(11-21-6-17(13-37-21)23(33)34)12-22(26)16-4-2-15(10-29)3-5-16/h2-9,13,22H,11-12,14H2,1H3,(H,33,34)/t22-,26+/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. In mouse splenocytes and a mouse ICAM-1 expressing cell lines, bEND, BMS-587101 shows inhibitory activities, with an IC50 of 150 nM.
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.
Products are for research use only. Not for human use.
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