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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)
Other Forms of PMX 53 acetate(219639-75-5 free base):
PMX-53T28429219639-75-5
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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 SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$113In StockIn Stock
5 mg$258In StockIn Stock
10 mg$382In StockIn Stock
25 mg$592In StockIn Stock
50 mg$816In StockIn Stock
100 mg$1,090In StockIn Stock
200 mg$1,480In StockIn Stock
1 mL x 10 mM (in DMSO)$398In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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.
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Batch Information

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Purity:99.91%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight956.16
FormulaC49H69N11O9
Cas No.852629-88-0
SmilesN=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
SequenceAc-Phe-Orn(1)-Pro-D-Cha-Trp-Arg-(1)
Sequence ShortFPWR
Storage & Solubility Information
Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
H2O: 95.6 mg/mL (99.98 mM), Sonication and heating are recommended.
DMSO: 125 mg/mL (130.73 mM), Sonication is recommended.
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM1.0459 mL5.2293 mL10.4585 mL52.2925 mL
5 mM0.2092 mL1.0459 mL2.0917 mL10.4585 mL
10 mM0.1046 mL0.5229 mL1.0459 mL5.2293 mL
20 mM0.0523 mL0.2615 mL0.5229 mL2.6146 mL
50 mM0.0209 mL0.1046 mL0.2092 mL1.0459 mL
DMSO
1mg5mg10mg50mg
100 mM0.0105 mL0.0523 mL0.1046 mL0.5229 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

PMX 53 acetate(219639-75-5 free base)PMX 53 acetate(219639755 free base)PMX 53 acetate(219639 75 5 free base)ComplementSystemComplement Systemcomplement 5a receptor (C5aR)
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