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PMX-53

Cat. No. M20998
PMX-53 Structure
Synonym:

3D53; PMX53; Ac-Phe-[Orn-Pro-dCha-Trp-Arg]

Size Price Availability Quantity
1mg USD 140  USD140 In stock
5mg USD 240  USD240 In stock
10mg USD 390  USD390 In stock
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Quality Control & Documentation
Biological Activity

PMX-53 is a potent CD88 (C5aR) antagonist with an IC50 of 20 nM, it inhibits C5a-induced neutrophil myeloperoxidase release and chemotaxis with IC50 values of 22 nM and 75 nM, respectively. 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 the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects.

Chemical Information
Molecular Weight 896.09
Formula C47H65N11O7
CAS Number 219639-75-5
Form Solid
Solubility (25°C) DMSO 100 mg/mL
Water 5 mg/mL (ultrasonic and warming)
Storage Store at ≤ -20°C, protect from light, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yubo Hou, et al. In Vitro Cell Dev Biol Anim. Gingipain of Porphyromonas gingivalis manipulates M1 macrophage polarization through C5a pathway

[2] George Hajishengallis, et al. Adv Exp Med Biol. Complement Involvement in Periodontitis: Molecular Mechanisms and Rational Therapeutic Approaches

[3] Haihui Wu, et al. Prog Histochem Cytochem. The Origin, Expression, Function and Future Research Focus of a G Protein-coupled Receptor, Mas-related Gene X2 (MrgX2)

[4] Hariharan Subramanian, et al. Mol Pharmacol. PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells

[5] E Ting, et al. Br J Pharmacol. Role of complement C5a in mechanical inflammatory hypernociception: potential use of C5a receptor antagonists to control inflammatory pain

[6] Jrg Khl. Curr Opin Mol Ther. Drug evaluation: the C5a receptor antagonist PMX-53

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  Catalog
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Keywords: PMX-53, 3D53; PMX53; Ac-Phe-[Orn-Pro-dCha-Trp-Arg] supplier, Complement System, inhibitors, activators


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