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PMX 53 acetate(219639-75-5 free base)
🥰Excellent
Catalog No. TP2334Cas No. 852629-88-0
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).
PMX 53 acetate(219639-75-5 free base)
🥰Excellent
Purity: 99.91%
Catalog No. TP2334Cas No. 852629-88-0
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 | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $113 | In Stock | |
| 5 mg | $258 | In Stock | |
| 10 mg | $382 | In Stock | |
| 25 mg | $592 | In Stock | |
| 50 mg | $816 | In Stock | |
| 100 mg | $1,090 | In Stock | |
| 200 mg | $1,480 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $398 | In Stock |
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Purity:99.91%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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 |
| Smiles | N=C(N)NCCC[C@@H]1NC([C@H](CC2=CNC3=C2C=CC=C3)NC([C@@H](CC4CCCCC4)NC([C@H]5N(C([C@H](CCCNC1=O)NC([C@H](CC6=CC=CC=C6)NC(C)=O)=O)=O)CCC5)=O)=O)=O.CC(O)=O |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 125 mg/mL (139.49 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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