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CXCR2-IN-2

    级别和纯度:
  • 10mM in DMSO
  • CAS编号: 1838123-21-9
  • 分子式: C18H23ClN2O5S
  • 分子量: 414.90
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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
C655405-1ml
1ml 期货 Stock Image

基本描述

规格或纯度 10mM in DMSO
英文名称 CXCR2-IN-2
生化机理 CXCR2-IN-2 是一种具有选择性、脑穿透性和口服生物利用度的 CXCR2 拮抗剂(β-arrestin 试验/CXCR2 Tango 试验的 IC 50 分别为 5.2 nM/1 nM)。与 CXCR1 相比,CXCR2-IN-2 的选择性约为 730 倍,与其他所有 CXCR2 拮抗剂相比,其选择性约为 1900 倍。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 拮抗剂
产品介绍


CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist ( IC 50 =5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC 50 of 0.04 μM

In Vivo

CXCR2-IN-2 (compound 68) (1-10 mg/kg; p.o.; twice daily for 3 days) dose-dependently reduces neutrophil infiltration in vivo in rat and mouse air pouch models . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-8 week old male C57Bl/6 mice (Air Pouch Model in Mouse) Dosage: 1, 3, and 10 mg/kg Administration: P.o.; twice daily for 3 days Result: Significantly inhibited neutrophil infiltration into mouse air pouch. Animal Model: 8-10 week old male Wistar rats (Air Pouch Model in Rat) Dosage: 1, 3, and 10 mg/kg Administration: P.o.; twice daily for 3 days Result: Inhibited neutrophil migration to air pouch in rat.

IC50& Target:CXCR2 5.2 nM (IC 50 ) CXCR1 3.8 μM (IC 50 )

关联靶点(人)

CXCR2 Tchem CXC 趋化因子受体 2 型(C-X-C chemokine receptor type 2) (4 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Isomeric SMILES CC1=CCC[C@H]1NC(=O)NC2=C(C(=C(C=C2)Cl)S(=O)(=O)[C@]3(CCOC3)C)O
PubChem CID 100951623
分子量 414.90

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