keep away from moisture
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 189.00 | |
5 mg | In stock | $ 430.00 | |
10 mg | In stock | $ 636.00 | |
25 mg | In stock | $ 987.00 | |
50 mg | In stock | $ 1,360.00 | |
100 mg | In stock | $ 1,830.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 665.00 |
Description | 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). |
In vitro | 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]. |
In vivo |
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]. |
Molecular Weight | 956.16 |
Formula | C49H69N11O9 |
CAS No. | 852629-88-0 |
keep away from moisture
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (139.49 mM), Sonification is recommended.
You can also refer to dose conversion for different animals. More
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PMX 53 acetate(219639-75-5 free base) 852629-88-0 Immunology/Inflammation Complement System PMX 53 acetate(219639755 free base) PMX 53 acetate(219639 75 5 free base) inhibitor inhibit