1. Immunology/Inflammation
  2. Complement System
  3. PMX-53

PMX-53 (Synonyms: 3D53)

Cat. No.: HY-106178
Handling Instructions

PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC50 of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to CaR2 and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects.

For research use only. We do not sell to patients.

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PMX-53 Chemical Structure

PMX-53 Chemical Structure

CAS No. : 219639-75-5

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Description

PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC50 of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to CaR2 and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects[1][2][3][4][5][6].

IC50 & Target

IC50: 20 nM (Complement C5a receptor)[4]
MrgX2[1]

In Vitro

PMX-53 is a potent CD88 antagonist and inhibits C5a-induced neutrophil myeloperoxidase release and chemotaxis with IC50 values of 22 nM and 75 nM, respectively[1].
PMX-53 (10 nM) inhibits C5a-induced Ca2+ mobilization in HMC-1 cells, 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 abolishes 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

PMX-53 (0.3-3 mg/kg; subcutaneous injection; once; male Wistar rats) treatment inhibits the hypernociception induced by zymosan-activated serum and C5a but not by the direct-acting hypernociceptive mediators, prostaglandin E2 and dopamine[2].
Local pretreatment of rats with PMX-53 (60-180 μg per paw) inhibits zymosan-, carrageenan-, lipopolysaccharide (LPS)- and antigen-induced hypernociception[2].
Pharmacokinetic analyses have shown that PMX-53 (3D53) appears in the plasma within 5 min of oral administration (3 mg/kg) to rats, with peak blood levels of approximately 0.3 µM beingreached within 20 min The plasma elimination half-life wasapproximately 70 min in this case[3].
The non-acetylated version of PMX-53 (3D53) binds to isolated mouse neutrophils with a Kd value of 30 nM (mouse C5a binds with a Kd value of 0.3 nM) and inhibits mouse C5a-induced chemotaxis with an IC50 value of 0.5 nM[3].

Animal Model: Adult male Wistar rats (weighing 180-200 g) injected with zymosan[2]
Dosage: 0.3 mg/kg, 1 mg/kg or 3 mg/kg
Administration: Subcutaneous injection; once
Result: Inhibited the hypernociception induced by zymosan-activated serum and C5a.
Molecular Weight

896.09

Formula

C₄₇H₆₅N₁₁O₇

CAS No.

219639-75-5

Sequence

{Phe}{Orn}{Pro}{d-Cha}{Trp}{Arg} (Lactam bridge: Orn2- Arg6)

Sequence Shortening

F-Orn-PAWR (Lactam bridge: Orn2- Arg6)

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

PMX-533D53PMX53PMX 53Complement SystemPeptidicC5aanaphylatoxinanti-inflammatorynon-toxicCD88MrgX2degranulationchemotaxishypernociceptionantiatheroscleroticanticancerInhibitorinhibitorinhibit

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