| 名称 | PMX 53 acetate(219639-75-5 free base) |
| 描述 | PMX-53 is a potent and orally active CD88 (C5aR) antagonist (IC50: 20 nM) and inhibits C5a-induced neutrophil myeloperoxidase release and chemotaxis with IC50 values of 22 nM and 75 nM, respectively. PMX-53 is also an agonist of Mas-related gene 2 (MrgX2). |
| 体外活性 | In HMC-1 cells, PMX-53 (10 nM) inhibits C5a-induced Ca2+ mobilization, but at higher concentrations( ≥30 nM) it causes degranulation in LAD2 mast cells, CD34+ cell-derived mast cells, and RBL-2H3 cells stably expressing MrgX2. Replacement of Trp with Ala and Arg with dArg eliminates the ability of PMX-53 to inhibit C5a-induced Ca2+ mobilization in HMC-1 cells and to cause degranulation in RBL-2H3 cells expressing MrgX2[1]. |
| 体内活性 | Local pretreatment of rats with PMX-53 (60-180?μg per paw) inhibits zymosan-, carrageenan-, lipopolysaccharide (LPS)- and antigen-induced hypernociception[2].
Pharmacokinetic analyses demonstrate that PMX-53 appears in the plasma within 5 min of oral administration (3 mg/kg) to rats, with peak blood levels of approximately 0.3 μM being reached within 20 min. The plasma elimination half-life was approximately 70 min in this case[3]. |
| 存储条件 | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 125 mg/mL (139.49 mM), Sonication is recommended.
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| 关键字 | PMX 53 acetate(219639-75-5 free base) | PMX 53 acetate(219639755 free base) | PMX 53 acetate(219639 75 5 free base) |
| 相关产品 | EG01377 2HCl | Iptacopan hydrochloride | SB290157 trifluoroacetate | BCX 1470 hydrochloride | Complement C5-IN-1 | ADH-503 | CP-289 | Dexamethasone | Cyclosporin A | 3-Phenoxybenzaldehyde |
| 相关库 | 经典已知活性库 | 多肽分子库 | 药物功能重定位化合物库 | 抑制剂库 | NO PAINS 化合物库 | 口服活性化合物库 | 临床期小分子药物库 | 已知活性化合物库 | 临床前化合物库 |
United States
