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产品别名
C5aR Antagonist, DF2593A-Calbiochem
(R)-4-(1-(4-(piperidin-1-yl)butanamido)ethyl)phenyl trifluoromethanesulfonate, C5aR Inhibitor, DF2593A, C5aR Blocker, DF2593A, C5a Receptor Antagonist, DF2593A
基本信息
| Empirical Formula【经验(实验)分子式】 | C18H25F3N2O4S |
| Molecular weight | 422.46 |
| General description【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). |
| Biochem/physiol Actions【生化/生理作用】 | Cell permeable: yes Primary Target C5aR |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. |
| Other Notes【其他说明】 | Moriconi, A., et al. 2014. PNAS.111, 16937. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze protect from light |
| color【颜色】 | white |
| solubility【溶解性】 | DMSO: 50 mg/mL |
| storage temp.【储存温度】 | −20℃ |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
