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SCH 563705 is a potent and orally available CXCR2 and CXCR1 antagonist, with IC 50 s of 1.3 nM, 7.3 nM and K i s of 1 and 3 nM, respectively. In Vitro SCH 563705 (Compound 16) is a potent and orally available CXCR2 and CXCR1 antagonist, with IC 50 s of 1.3 nM, 7.3 nM and K i s of 1 and 3 nM, respectively. SCH 563705 shows potent inhibition against both Gro-a and IL-8 induced human neutrophil migration (chemotaxis IC 50 = 0.5 nM, against 30 nM of Gro-a; chemotaxis IC 50 = 37 nM, against 3 nM of IL-8). SCH 563705 potently inhibits mouse CXCR2 (IC 50 = 5.2 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo SCH 563705 has good oral pharmacokinetic profiles in rats, mice, monkeys and dogs . SCH 563705 (50 mg/kg p.o) reduces blood Ly6G + Ly6C + neutrophil frequency and unchanged levels of Ly6GLy6Chi monocytes. SCH563705 (3-30 mg/kg p.o) treatment causes a dosedependent elevation in plasma levels of CXCL1. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal administration Mice Induction of anti-collagen antibody-induced arthritis. Anti-collagen antibody-induced arthritis (ABIA) is induced in BALB/c mice (n = 8 mice per treatment group) as follows. On day 0, mice are injected intraperitoneally with 4 mg ArthritoMAB Arthritis-inducing Antibody Cocktail. On day 3, mice are boosted intraperitoneally with 50 μg of lipopolysaccharide from Escherichia coli 055:B5 in 200 μL sterile PBS. In all studies, SCH 563705 is administered in a vehicle consisting of 0.4% METHOCEL E15 premium hydroxypropyl methylcellulose (MC) . Clinical scores are determined daily as follows. Each paw is assigned a score of 0-4 based on the following criteria: asymptomatic, 0; slight redness, 1; one or more swollen digits in addition to redness, 2; swelling of entire paw, 3; ankylosing of joints and residing of swelling, 4. The sum of the four paw scores for each mouse (0-16) are plotted against time to calculate the area under the curve (AUC) of disease activity. Paw hickness measurements are made daily using a micrometer caliper over the metatarsals of the paw. The percent change in paw thickness relative to baseline (day 0) measurements is then calculated . aladdin has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:CXCR2 1 nM (Ki) CXCR1 3 nM (Ki) CXCR2 1.3 nM (IC 50 ) CXCR1 7.3 nM (IC 50 ) Mouse CXCR2 5.2 nM (IC 50 )
中文名称
SCH 563705
英文名称
SCH 563705
中文别名
-
英文别名
MS-27493 | AKOS016009722 | CC(C1=COC([C@H](NC2=C(C(C2=O)=O)NC3=CC=CC(C(N(C)C)=O)=C3O)CC)=C1)C | SCH-563705 | NCGC00379077-01 | AKOS015856220 | SCH 563705 | DTXSID90437927 | 3-[[3,4-Dioxo-2-[[(1R)-1-(4-propan-2-ylfuran-2-yl)propyl]amino]cyclobuten-1-yl]ami
CAS号
473728-58-4
分子式
C23H27N3O5
分子量
425.48 g/mol
精确质量
-
PSA
112.000 Ų
Logp
3.800
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SCH 563705 5mg

品牌:阿拉丁
货号:S649455-5mg
级别: -
货期:30天
已售 135 件
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5mg

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