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C5aR Antagonist, DF2593A-Calbiochem

品牌
Sigma-Aldrich
货号
5.33797
包装型号
规格纯度
参考价格
1966.13 *本价格含增值税费
促销
数量
-+
产品介绍:

产品说明

一般描述

An orally available, blood-brain barrier permeant piperidinylbutanamide compound that acts as a highly potent, selective, non-competitive and allosteric antagonist of C5a receptor (C5aR). Shown to effectively block C5a-induced human PMN migration (IC50 = 5.0 nM) and is also effective in rat and mouse orthologs (IC50 = 6.0 and 1 nM for rat and mouse, respectively). Exhibits good selectivity against a panel of GPCRs and ion channels screened and is shown to be completely inactive in a prostaglandin E2 production assay (~10 µM). Blocks C5a-induced and carrageenan-induced hyperalgesia in mice without any sedative or central opioid-like effects. Following oral administration, it is rapidly absorbed and displays favorable pharmacokinetic profile (Cmax = 100 nM; Tmax = 1.2 h at 1 mg/kg in mice).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
An orally available, blood-brain barrier permeant piperidinylbutanamide compound that acts as a highly potent, selective, non-competitive and allosteric antagonist of C5a receptor (C5aR). Shown to effectively block C5a-induced human PMN migration (IC50 = 5.0 nM) and is also effective in rat and mouse orthologs (IC50 = 6.0 and 1 nM for rat and mouse, respectively). Exhibits good selectivity against a panel of GPCRs and ion channels screened and is shown to be completely inactive in a prostaglandin E2 production assay (~10 µM). Blocks C5a-induced and carrageenan-induced hyperalgesia in mice without any sedative or central opioid-like effects. Following oral administration, it is rapidly absorbed and displays favorable pharmacokinetic profile (Cmax = 100 nM; Tmax = 1.2 h at 1 mg/kg in mice).

生化/生理作用

Cell permeable: yes
Primary Target
C5aR

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Moriconi, A., et al. 2014. PNAS.111, 16937.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式C18H25F3N2O4S
分子量422.46

产品性质

质量水平100
测定≥98% (HPLC)
形式solid
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 white
溶解性DMSO: 50 mg/mL
储存温度−20℃

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

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