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CCR2 antagonist 5
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CCR2 antagonist 5图片
CAS NO:1228650-83-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
CCR2 antagonist 5 是一种选择性的口服活性hCCR2抑制剂,具有良好的结合亲和力 (IC50=37 nM) 和有效的功能拮抗作用 (chemotaxis IC50=30 nM)。CCR2 antagonist 5 对 mCCR2 结合的 Ki为 9.6 μM。CCR2 antagonist 5 可用于炎症性疾病的研究。
生物活性

CCR2 antagonist5 is a selective, orally activehCCR2inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM).CCR2 antagonist5 displays a Kiof 9.6 μM for mCCR2 binding.CCR2 antagonist5 can be used in the research of inflammatory disease[1].

IC50& Target[1]

hCCR2

37 nM (IC50)

mCCR2

9.6 μM (Ki)

体内研究
(In Vivo)

CCR2 antagonist 5 (compound 8d) dose-dependently inhibits the influx of leukocytes, monocytes/macrophages and T-lymphocytes into the peritoneal cavity with an ED50of 3 mg/kg p.o. bid in a thioglycollate-induced peritonitis (TG) model[1].
CCR2 antagonist 5 has good CV safety profile. It does not induce dose-dependent or notable effects on most cardiohemodynamic, functional respiratory and electrophysiological parameters up to 10 mg/kg (i.v.) with plasma level at 70 μM in an anesthetized dog[1].
CCR2 antagonist 5 has amendable oral bioavailability in dogs and primates. Pharmacokinetic parameters (p.o.)[1]:

SpeciesDose
(mg/kg)
Cmax
(ng/mL)
AUClast
(h*ng/mL)
Oral bioavailability
(%)
dogs6.71617588770.2
non-human primates7.2740306125.4
mice107420419
rats1010041615.3

分子量

482.52

Formula

C22H25F3N4O3S

CAS 号

1228650-83-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.