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PMX 53 acetate(219639-75-5 free base)

Catalog No. TP2334 CAS 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).

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PMX 53 acetate(219639-75-5 free base) Chemical Structure

PMX 53 acetate(219639-75-5 free base), CAS 852629-88-0

Pack Size	Availability	Price/USD
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

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Purity: 99.91%

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Storage & Solubility Information

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

Storage

keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (139.49 mM), Sonification is recommended.

References and Literature

1. Subramanian H, et al. PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells. Mol Pharmacol. 2011 Jun;79(6):1005-13. 2. Ting E, et al. Role of complement C5a in mechanical inflammatory hypernociception: potential use of C5a receptor antagonists to control inflammatory pain. Br J Pharmacol. 2008 Mar;153(5):1043-53. 3. Holland MC, et al. Synthetic small-molecule complement inhibitors. Curr Opin Investig Drugs. 2004 Nov;5(11):1164-73. 4. Finch AM, et al. Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a. J Med Chem. 1999 Jun 3;42(11):1965-74.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library Peptide Compound Library Orally Active Compound Library NO PAINS Compound Library Bioactive Compound Library Immunology/Inflammation Compound Library Clinical Compound Library Bioactive Compounds Library Max Preclinical Compound Library

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Keywords

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

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