PMX-53
Based on 9 publication(s) in Google Scholar
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 the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects.
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- Purity: 99.95%
- CAS No.: 219639-75-5
- 화학식: C47H65N11O7
- 분자량:896.09
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보관:
-20°C, sealed storage, away from moisture and light, under nitrogen
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light, under nitrogen)
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Biological Activity
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Chemical Information
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- References
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Publications Citing Use of MedChemExpress (MCE) PMX-53
More- Nat Commun. 2024 May 27;15(1):4485. [Abstract]
- Neuron. 2025 Oct 24:S0896-6273(25)00751-2. [Abstract]
- Mol Ther. 2023 Aug 2;31(8):2507-2523. [Abstract]
- Int Immunopharmacol. 2024 Apr 20:131:111874. [Abstract]
- Invest Ophthalmol Vis Sci. 2026 Feb 2;67(2):35. [Abstract]
- Brain Res Bull. 2026 May 20:111941. [Abstract]
- J Cell Commun Signal. 2025 Dec 19;19(4):e70055. [Abstract]
- Justus Liebig University Giessen. 2026.
- Research Square Print. November 28th, 2022.
Customer Validation & Images
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Bio/Physico-chemical Assay
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WB
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
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In Vivo Efficacy Study
Biological Activity
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
0.104 μM
Compound: 1, PMX53
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Inhibition of C5a binding to human C5aR expressed in HEK293 cells
Inhibition of C5a binding to human C5aR expressed in HEK293 cells
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[PMID: 16876401] |
| J774.A1 | IC50 |
7.1 μM
Compound: 1, PMX53
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Inhibition of C5a-induced chemotaxis of mouse J774A.1 cells
Inhibition of C5a-induced chemotaxis of mouse J774A.1 cells
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[PMID: 16876401] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 being reached within 20 min The plasma elimination half-life was approximately 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male Wistar rats (weighing 180-200 g) injected with zymosan[2]
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Dosage:0.3 mg/kg, 1 mg/kg or 3 mg/kg
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Administration:Subcutaneous injection; once
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Result:Inhibited the hypernociception induced by zymosan-activated serum and C5a.
Chemical Information
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CAS No. 219639-75-5
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Appearance Solid
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분자량 896.09
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화학식 C47H65N11O7
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Color White to off-white
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Synonyms
3D53
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Sequence
Ac-Phe-{Orn}-Pro-{dCha}-Trp-Arg (Lactam bridge: Orn2-Arg6)
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Sequence Shortening
Ac-F-{Orn}-P-{dCha}-WR (Lactam bridge: Orn2-Arg6)
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, sealed storage, away from moisture and light, under nitrogen
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light, under nitrogen)
Publications (9)
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Journal Impact Factor
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Most Recent
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Nat Commun
C5aR1 inhibition reprograms tumor associated macrophages and reverses PARP inhibitor resistance in breast cancer. [Abstract]2024 May 27;15(1):4485. PMID: 38802355 -
Neuron
BST2 expression at astrocyte borders promotes microglial recruitment via the C3/C3aR signaling. [Abstract]2025 Oct 24:S0896-6273(25)00751-2. PMID: 41138733 -
Mol Ther
2023 Aug 2;31(8):2507-2523. PMID: 37143324
PMX-53 purchased from MedChemExpress. Usage Cited in: Mol Ther. 2023 Aug 2;31(8):2507-2523. [Abstract]
Chemotaxis of THP1 cells toward medium without FBS (control), medium without FBS + 0.1 μg/mL of C5a (C5a), and THP1 cells pre-treated 30 min with 0.9 μg/mL PMX53 toward medium without FBS + 0.1 μg/mL C5a (PMX53 + C5a) was evaluated. After 2 h of migration, RFU (Ex/Em = 485/520 nm) was measured.
PMX-53 purchased from MedChemExpress. Usage Cited in: Mol Ther. 2023 Aug 2;31(8):2507-2523. [Abstract]
Western blotting of phosphoS6, phosphoHSP27, phosphoERK, and the loading control β-actin of THP1 cells untreated or treated with PMX53 (0.9 μg/mL) and/or C5a for 30 min. The experiment was performed three times with similar results.
PMX-53 purchased from MedChemExpress. Usage Cited in: Mol Ther. 2023 Aug 2;31(8):2507-2523. [Abstract]
Chemotaxis of primary monocytes isolated from WT and C5aR1-/- mice toward medium without FBS, medium without FBS + 0.1 μg/mL of C5a (C5a). Migration of WT monocytes pre-treated for 30 min with 0.9 μg/mL PMX53 toward medium without FBS + 0.1 μg/mL C5a was also evaluated n = 4–6.
PMX-53 purchased from MedChemExpress. Usage Cited in: Mol Ther. 2023 Aug 2;31(8):2507-2523. [Abstract]
Schematic representation of the pharmacological inhibition of C5aR1 in the DoxoR-induced senescence model. At day 0, 15-week-old mice received either vehicle or DoxoR (10 mg/kg, i.p.). From day 1 to day 30, mice received PMX53 (1 mg/kg, daily subcutaneous) or vehicle 2.
PMX-53 purchased from MedChemExpress. Usage Cited in: Mol Ther. 2023 Aug 2;31(8):2507-2523. [Abstract]
Schematic representation of the pharmacological inhibition of C5aR1 in the DoxoR-induced senescence model. At day 0, 15-week-old mice received either vehicle or DoxoR (10 mg/kg, i.p.). From day 1 to day 30, mice received PMX53 (1 mg/kg, daily subcutaneous) or vehicle 2. Quantitative parameters and 3D representation of the cortical bone of tibiae measured by μ-CT.
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Int Immunopharmacol
Bulk and single-cell RNA sequencing analysis with 101 machine learning combinations reveal neutrophil extracellular trap involvement in hepatic ischemia-reperfusion injury and early allograft dysfunction. [Abstract]2024 Apr 20:131:111874. PMID: 38493695 -
Invest Ophthalmol Vis Sci
The Intracellular C5a-mtC5aR1 Axis Promotes Necroptosis in Dry Eye Through DRP1-Mediated Mitochondrial Dysfunction. [Abstract]2026 Feb 2;67(2):35. PMID: 41705776 -
Brain Res Bull
Inhibition of C5aR1 alleviates early brain injury after subarachnoid hemorrhage by reducing STAT3 phosphorylation and attenuating neuroinflammation. [Abstract]2026 May 20:111941. PMID: 42167499 -
J Cell Commun Signal
Regulation of phosphatase and tensin homolog by complement component 5a (C5a) and its receptor (C5aR1) in lupus nephritis: A novel therapeutic target. [Abstract]2025 Dec 19;19(4):e70055. PMID: 41426360 -
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용액&용해도
DMSO : 100 mg/mL (111.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 50 mg/mL (55.80 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (2.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (2.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
순도&문서
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Data Sheet (287 KB)
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SDS (252 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
[3]. Holland MC, et al. Synthetic small-molecule complement inhibitors. Curr Opin Investig Drugs. 2004 Nov;5(11):1164-73. [Content Brief]
[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. [Content Brief]
[5]. Manthey HD, et al. Complement C5a inhibition reduces atherosclerosis in ApoE-/- mice. FASEB J. 2011 Jul;25(7):2447-55. [Content Brief]
[6]. Vadrevu SK, et al. Complement c5a receptor facilitates cancer metastasis by altering T-cell responses in the metastatic niche. Cancer Res. 2014 Jul 1;74(13):3454-65. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.1160 mL | 5.5798 mL | 11.1596 mL | 27.8990 mL |
| 5 mM | 0.2232 mL | 1.1160 mL | 2.2319 mL | 5.5798 mL | |
| 10 mM | 0.1116 mL | 0.5580 mL | 1.1160 mL | 2.7899 mL | |
| 15 mM | 0.0744 mL | 0.3720 mL | 0.7440 mL | 1.8599 mL | |
| 20 mM | 0.0558 mL | 0.2790 mL | 0.5580 mL | 1.3949 mL | |
| 25 mM | 0.0446 mL | 0.2232 mL | 0.4464 mL | 1.1160 mL | |
| 30 mM | 0.0372 mL | 0.1860 mL | 0.3720 mL | 0.9300 mL | |
| 40 mM | 0.0279 mL | 0.1395 mL | 0.2790 mL | 0.6975 mL | |
| 50 mM | 0.0223 mL | 0.1116 mL | 0.2232 mL | 0.5580 mL | |
| DMSO | 60 mM | 0.0186 mL | 0.0930 mL | 0.1860 mL | 0.4650 mL |
| 80 mM | 0.0139 mL | 0.0697 mL | 0.1395 mL | 0.3487 mL | |
| 100 mM | 0.0112 mL | 0.0558 mL | 0.1116 mL | 0.2790 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
PMX-53 Related Classifications
HY-106178 Related Classifications
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