| Field | Specification |
|---|---|
| Applications | |
| Molecular weight | |
| Molecular formula | C47H63F3N10O8 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
PMX 205 Trifluoroacetate is a specific antagonist of the complement C5aR1 isoform[1][2][3][4]. The manufacturer groups this compound under its Immunology/Inflammation pathway category.
It is supplied by the manufacturer as a white to off-white solid, with a molecular formula of C47H63F3N10O8, a molecular weight of 953.06 g/mol, and a purity of 99.50%.
Physical & Chemical Properties
| Molecular Formula | C47H63F3N10O8 |
|---|---|
| Molecular Weight | 953.06 g/mol |
| Purity | 99.50% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | OC(C(F)(F)F)=O.O=C([C@H](NC([C@@]1([H])N(CCC1)C([C@](NC(CCC2=CC=CC=C2)=O)([H])CCCNC([C@H](CCCNC(N)=N)NC3=O)=O)=O)=O)CC4CCCCC4)N[C@@]3([H])CC5=CNC6=CC=CC=C56 |
| Signaling Pathway | Immunology/Inflammation |
| Solubility | In Vitro: DMSO: ≥ 100 mg/mL (104.93 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O: < 0.1 mg/mL (insoluble) * "≥" means soluble, but saturation unknown. |
| Storage | -20°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | ≥ 100 mg/mL (104.93 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
| H2O | < 0.1 mg/mL | insoluble |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (2.62 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (2.62 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (2.62 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
The complement activation product C5a is known to recruit and activate microglia and astrocytes in vitro through activation of a G protein-coupled cell-surface C5aR. In the MTT assay on the 24 h plate, all groups differ significantly from the negative control group. The value recorded is between 0.09893 to 0.2465 for the PMX 205 (PMX205) group, 0.02724 to 0.1748 for the EP54 group, and 0.09880 to 0.2464 for the Tamoxifen group. On the plate incubated for 48 h, only two groups show a significant result, PMX 205 and Tamoxifen, with recorded values between 0.04987 to 0.3273 and 0.5777 to 0.8551, respectively. On the 72 h plate, only one group, PMX 205 (antagonist group), shows a significant result, with the value recorded between 0.02136 to 0.5322[1].
In Vivo
PMX 205 (PMX205) acts as a selective, orally active C5aR antagonist. In rats, oral PMX 205 (1 mg/kg/day) markedly extends survival time and lowers end-stage motor scores relative to vehicle-treated rats, and treated animals also show lower levels of astroglial proliferation in the lumbar spinal cord. SOD1G93A rats receive oral PMX 205 (1 mg/kg/day) starting at one of two time points (days 28 and 70), ahead of the onset of major clinical symptoms. Survival time is significantly extended in both treatment groups versus untreated rats (p=0.022, day 28; p=0.015, day 70), and the two treatment regimens do not clearly differ in outcome[2]. Tg2576 mice receive PMX 205 (PMX205) at 20 μg/mL in drinking water (n=17) from 12 to 15 mo of age, a period of rapid amyloid deposit accumulation in these animals, while untreated Tg2576 animals (n=11) serve as controls. After 3 mo, PMX 205-treated animals have significantly lower fibrillar plaque load (thioflavine reactivity) than untreated animals. PMX 205 also significantly lowers hyperphosphorylated tau (69%) in 3×Tg mice[3].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay[1]
Plate mouse mammary tumor 4T1 cells at 5.0×104 cells/ml/well in 96-multiwell plates in complete medium. Incubate for 24 h, then replace the medium with serum-starve medium to synchronize the cell cycle and growth so that the cells reach their plateau phase. After 24 h of serum starvation, treat the cells with 5 μL/well of 0.1 M agonist, EP54, antagonist, PMX 205, and treat the positive control with Tamoxifen. Add 5 μL/well of the 12 mM ck solution 5 h before reading, and add about 50 μL/well of the SDS-HCL solution, mixing thoroughly by pipette, 3 h before reading. Run the MTT assay at 0, 24, 48 and 72 h, measuring at 570 nm with an ELISA plate reader Infinite M200[1].
Animal Administration[2][3]
Rats[2] Use transgenic SOD1G93A rats expressing human mutant G93A SOD1 (NTac:SD-Tg SOD1G93A L26H). Set up three experimental groups: untreated, PMX 205 from day 28 onward, and PMX 205 from day 70 onward. Give PMX 205 in drinking water (1 mg/kg/day) from day 28 or day 70 onward, and give controls water only[2]. Mice[3] Treat Tg2576 mice for 2-3 mo (starting at or after the initiation of plaque pathology) with PMX 205 in drinking water alone (10-20 μg/mL, equivalent to ~3-6 mg/kg/day), or in drinking water (10-20 μg/mL) combined with s.c. dosing (1 mg/kg) twice weekly throughout the treatment period. Use untreated transgenic animals of the same age as controls. Treat nontransgenic littermates with or without the drug in the same way. Also treat 3×Tg mice with PMX 205 in drinking water. Use only female mice of this strain because of the low pathology in males[3].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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NNMT inhibition in cancer-associated fibroblasts restores antitumour immunity. Nature 2025 Sep;645(8082):1051-1059. PMID: 40702186
The hepatocyte-specifically expressed lnc-HSER alleviates hepatic fibrosis by inhibiting hepatocyte apoptosis and epithelial-mesenchymal transition. Theranostics 2019 Oct 12;9(25):7566-7582.
Neutrophil-microglia interaction drives motor dysfunction in a neuromyelitis optica model induced by subarachnoid AQP4-IgG. J Clin Invest 2026 Feb 10:e199706. PMID: 41665955
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Intracellular C5aR1 inhibits ferroptosis in glioblastoma through METTL3-dependent m6A methylation of GPX4. Cell Death Dis 2024 Oct 5;15(10):729. PMID: 39368999
Complement C5a/C5aR1 pathway facilitates glioblastoma progression via fostering glioma stem cell-macrophage symbiosis. J Neuroinflammation 2026 Jun 24. PMID: 42343442
Anti-PLA2R antibodies promote endothelial pyroptosis and a procoagulant phenotype through FcγRI signaling. Nephrol Dial Transplant 2026 May 13:gfag109. PMID: 42127088
Physical exercise modulates the microglial complement pathway in mice to relieve cortical circuitry deficits induced by mutant human TDP-43. Cell Rep 2023 Mar 15;42(3):112240. PMID: 36924491
Mild Hypothermia Alleviates Complement C5a-Induced Neuronal Autophagy During Brain Ischemia-Reperfusion Injury After Cardiac Arrest. Cell Mol Neurobiol 2023 Jul;43(5):1957-1974. PMID: 36006573
The Crosstalk Between Sepsis-Associated Encephalopathy and Alzheimer's Disease: Identifying Potential Biomarkers and Therapeutic Targets for Cognition. Mol Neurobiol 2025 Jul 10. PMID: 40634788
