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BMS-688521 Sale

目录号 : GC38893

BMS-688521 是一种高效、具有口服活性的 LFA-1/ICAM 相互作用抑制剂,在粘附试验中 IC50 为 2.5 nM,在 MLR 试验中 IC50 为 60 nM。BMS-688521 对小鼠变应性嗜酸性肺炎模型有较好的治疗作用。

BMS-688521 Chemical Structure

Cas No.:893397-44-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥6,903.00
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5mg
¥5,850.00
现货
10mg
¥9,360.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

BMS-688521 is a highly potent, orally active inhibitor of the LFA-1/ICAM interaction, with an IC50 of 2.5 nM in the adhesion assay and an IC50 of 60 nM in the MLR assay. BMS-688521 is efficacious in a mouse allergic eosinophilic lung inflammation model[1].

BMS-688521 in a mouse specific adhesion assay employed mouse splenocytes and a mouse ICAM-1 expression cell line, b.END3. BMS-688521 has an IC50 of 78 nM, representing an approximately 30-fold decrease in activity relative to the human T-cell/HUVEC assay data (ICIC50=2.5 nM)[1].

BMS-688521 (1-10 mg/kg; p.o.; BID for a three-day) is efficacious in a mouse allergic eosinophilic lung inflammation model[1].BMS-688521 (5 mg/kg; p.o.) treatment shows the Cmax, Tmax, AUC, F values are 0.32 μM, 1.0 μM, 1.5 μM h, and 50%, respectively[1].BMS-688521 (1 mg/kg; i.v.) treatment shows the T1/2, MRT, CL and Vss values are 1.6 hours, 1.7 hours, 50 mL/mim/kg, and 5.1 L/kg, respectively in BALB/c mice[1]. Animal Model: BALB/c female mice, 6-8 week of age (OVA Lung Inflammation in Mice)[1]

[1]. Watterson SH, et al. Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic acid (BMS-688521). J Med Chem. 2010 May 13;53(9):3814-30.

Chemical Properties

Cas No. 893397-44-9 SDF
Canonical SMILES ClC1=CC(Cl)=CC(N(C(N(C)[C@]23[C@H](C4=CC=C(C#N)C=C4)CN(C5=NC=C(C(O)=O)C=C5)C3)=O)C2=O)=C1
分子式 C26H19Cl2N5O4 分子量 536.37
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mM 1.8644 mL 9.3219 mL 18.6438 mL
5 mM 0.3729 mL 1.8644 mL 3.7288 mL
10 mM 0.1864 mL 0.9322 mL 1.8644 mL
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Research Update

Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic acid (BMS-688521)

J Med Chem 2010 May 13;53(9):3814-30.PMID:20405922DOI:10.1021/jm100348u

Leukocyte function-associated antigen-1 (LFA-1), also known as CD11a/CD18 or alpha(L)beta(2), belongs to the beta(2) integrin subfamily and is constitutively expressed on all leukocytes. The major ligands of LFA-1 include three intercellular adhesion molecules 1, 2, and 3 (ICAM 1, 2, and 3). The interactions between LFA-1 and the ICAMs are critical for cell adhesion, and preclinical animal studies and clinical data from the humanized anti-LFA-1 antibody efalizumab have provided proof-of-concept for LFA-1 as an immunological target. This article will detail the structure-activity relationships (SAR) leading to a novel second generation series of highly potent spirocyclic hydantoin antagonists of LFA-1. With significantly enhanced in vitro and ex vivo potency relative to our first clinical compound (1), as well as demonstrated in vivo activity and an acceptable pharmacokinetic and safety profile, 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro-[4.4]nonan-7-yl)nicotinic acid (2e) was selected to advance into clinical trials.