Cat. No.: HY-110136

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PMX 205

14 Cited Publications

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Based on 14 publication(s) in Google Scholar

PMX 205 is a potent complement C5a receptor (C5aR; CD88) antagonist.

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Pureté: 99.95%
CAS No.: 514814-49-4
Formule: C₄₅H₆₂N₁₀O₆
Masse moléculaire:839.04

Stockage:

Sealed storage, away from moisture.

Powder -80°C, 2 years , -20°C, 1 year

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

PMX 205 Chemical Structure

CAS No.: 514814-49-4

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (14)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

PMX 205 is a potent complement C5a receptor (C5aR; CD88) antagonist.

IC₅₀ & Target

C5aR^[1]

In Vitro

A complement activation product, C5a, is known to recruit and activate microglia and astrocytes in vitro by activation of a G protein-coupled cell-surface C5aR. In the MTT assay, in 24 h plate, it shows that all groups are significant when compared with negative control group. For PMX 205 (PMX205) group, the value recorded is in between 0.09893 to 0.2465, EP54 group, 0.02724 to 0.1748 and Tamoxifen group, the value recorded in between 0.09880 to 0.2464. For the 48 h plate of incubation time, only two groups show a significant result, which are PMX 205 and Tamoxifen. The values recorded are in between 0.04987 to 0.3273 and 0.5777 to 0.8551 respectively. For the 72 h plate, only one group shows a significant result, PMX 205 (antagonist group) with the value recorded in between 0.02136 to 0.5322^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PMX 205 (PMX205) is an orally active, selective C5aR antagonist. Animals treated with PMX 205 (1 mg/kg/day, oral) displays a significant extension of survival time and a reduction in end-stage motor scores, as compared with vehicle-treated rats. PMX 205-treated animals also display reduced levels of astroglial proliferation in the lumbar spinal cord. SOD1^G93A rats are orally dosed with PMX 205 (1 mg/kg/day) from two time points (days 28 and 70) before the onset of major clinical symptoms. Both treatment groups have a significant extension in survival time compared with untreated rats (p=0.022, day 28; p=0.015, day 70), with no clear differences in outcomes between the two treatment regimens^[2]. Tg2576 mice are treated with PMX 205 (PMX205) at 20 μg/mL in the drinking water (n=17) from 12 to 15 mo of age, the time frame at which there is a rapid accumulation of amyloid deposits in these animals. Untreated Tg2576 animals (n=11) are used as controls. After 3 mo, animals treated with PMX 205 show significantly less fibrillar plaque load (thioflavine reactivity) than do untreated animals. In 3×Tg mice, PMX 205 also significantly reduces hyperphosphorylated tau (69%)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 514814-49-4
Appearance Solid
Masse moléculaire 839.04
Formule C₄₅H₆₂N₁₀O₆
Color White to off-white
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (14)

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Journal Impact Factor

Nature

NNMT inhibition in cancer-associated fibroblasts restores antitumour immunity. [Abstract]

2025 Sep;645(8082):1051-1059. PMID: 40702186
Theranostics

The hepatocyte-specifically expressed lnc-HSER alleviates hepatic fibrosis by inhibiting hepatocyte apoptosis and epithelial-mesenchymal transition. [Abstract]

2019 Oct 12;9(25):7566-7582. PMID: 31695787
J Clin Invest

Neutrophil-microglia interaction drives motor dysfunction in a neuromyelitis optica model induced by subarachnoid AQP4-IgG. [Abstract]

2026 Feb 10:e199706. PMID: 41665955
Adv Sci (Weinh)

CD9 Counteracts Liver Steatosis and Mediates GCGR Agonist Hepatic Effects. [Abstract]

2024 Aug;11(29):e2400819. PMID: 38837628
Cell Death Dis

Intracellular C5aR1 inhibits ferroptosis in glioblastoma through METTL3-dependent m6A methylation of GPX4. [Abstract]

2024 Oct 5;15(10):729. PMID: 39368999

PMX 205 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Oct 5;15(10):729. [Abstract]

Protein expression of GPX4 after treatment with different concentrations of PMX205 (12 h) and the related quantitative analysis.

PMX 205 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Oct 5;15(10):729. [Abstract]

Representative bioluminescence images acquired by IVIS imaging showing luciferase signals in tumors of mice in the different treatment groups (PMX205: intraperitoneal injection, 5 mg/kg every two days for four weeks) at 1 week, 3 weeks, and 5 weeks.

PMX 205 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Oct 5;15(10):729. [Abstract]

IHC staining confirmed that PMX205 (intraperitoneal injection, 5 mg/kg every two days for four weeks) induced suppression of GPX4 expression, accumulation of 4-HNE, and inhibition of tumor growth.

PMX 205 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Oct 5;15(10):729. [Abstract]

PMX205 (intraperitoneal injection, 5 mg/kg every two days for four weeks) induced significant decreases in GPX4 protein expression.
Nephrol Dial Transplant

Anti-PLA2R antibodies promote endothelial pyroptosis and a procoagulant phenotype through FcγRI signaling. [Abstract]

2026 May 13:gfag109. PMID: 42127088
Cell Rep

Physical exercise modulates the microglial complement pathway in mice to relieve cortical circuitry deficits induced by mutant human TDP-43. [Abstract]

2023 Mar 15;42(3):112240. PMID: 36924491
Cell Mol Neurobiol

Mild Hypothermia Alleviates Complement C5a-Induced Neuronal Autophagy During Brain Ischemia-Reperfusion Injury After Cardiac Arrest. [Abstract]

2023 Jul;43(5):1957-1974. PMID: 36006573
Mol Neurobiol

The Crosstalk Between Sepsis-Associated Encephalopathy and Alzheimer's Disease: Identifying Potential Biomarkers and Therapeutic Targets for Cognition. [Abstract]

2025 Jul 10. PMID: 40634788
Int J Cancer

Complement receptor C5aR1 blockade reprograms tumor-associated macrophages and synergizes with anti-PD-1 therapy in gastric cancer. [Abstract]

2023 Jul 1;153(1):224-237. PMID: 36799619
Clin Immunol

Complement C5a and C5a receptor 1 mediates glomerular damage in focal segmental glomerulosclerosis. [Abstract]

2025 Apr:273:110459. PMID: 39984108

PMX 205 purchased from MedChemExpress. Usage Cited in: Clin Immunol. 2025 Apr:273:110459. [Abstract]

C5a (100 ng/ml, 48 h) stimulation increased CD44 expression in PECs at the protein level, effects that were blocked by PMX205 (5, 50, and 500 ng/ml, 48 h) in a dose-dependent manner.

PMX 205 purchased from MedChemExpress. Usage Cited in: Clin Immunol. 2025 Apr:273:110459. [Abstract]

C5a (100 ng/ml, 48 h) stimulation increased CD44 expression in PECs at the mRNA level, effects that were blocked by PMX205 (5, 50, and 500 ng/ml, 48 h) in a dose-dependent manner.

PMX 205 purchased from MedChemExpress. Usage Cited in: Clin Immunol. 2025 Apr:273:110459. [Abstract]

C5a (100 ng/ml, 48 h) exposure increased PEC-derived COL4A2 secretion and mRNA levels. This effect was reversed by PMX205 (5, 50, and 500 ng/ml, 48 h) in a dose-dependent manner.

PMX 205 purchased from MedChemExpress. Usage Cited in: Clin Immunol. 2025 Apr:273:110459. [Abstract]

The proliferation of PECs increased by C5a (100 ng/ml, 48 h) was reduced by PMX205 (5, 50, and 500 ng/ml, 48 h) in a dose-dependent manner.
bioRxiv

2026 Jun 16.
bioRxiv

Neutrophil-microglia interaction drives reversible motor dysfunction in neuromyelitis optica model induced by subarachnoid AQP4-IgG. [Abstract]

2025 Aug 28:2025.08.22.671883. PMID: 40909582
La Trobe University

2022 Jan.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (119.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.1918 mL

5.9592 mL

11.9184 mL

5 mM

0.2384 mL

1.1918 mL

2.3837 mL

10 mM

0.1192 mL

0.5959 mL

1.1918 mL

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (5.96 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (5.96 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (5.96 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[1]

The mouse mammary tumor cell lines 4T1 are plated at a density 5.0×10⁴ cells/ml/well of 96-multiwell plates in complete medium. After 24 h of incubation, the medium is changed with serum starve medium to synchronize the cell cycle and growth as to ensure that the cells reaches its plateau phase. After 24 h of serum-starving, cells are treated with 5 μL/well of 0.1 M of agonist, EP54, antagonist, PMX 205 and the positive control is treated with Tamoxifen drug. 5 μL/well of the 12 mM ck solution is added 5 h before reading is taken and about 50 μL/well of the SDS-HCL solution is added and mixed thoroughly using pipette 3 h before reading is taken. The MTT assay is assessed at different time point; 0, 24, 48 and 72 h at wavelength 570 nm respectively by using ELISA plate reader Infinite M200^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]^[3]

Rats^[2]
Transgenic SOD1^G93A rats expressing human mutant G93A SOD1 (NTac:SD-Tg SOD1^G93A L26H) are used. Three experimental groups are chosen: untreated, PMX 205 treats from day 28 onward, and PMX 205 treats from day 70 onward. Animals are administered PMX 205 via drinking water (1 mg/kg/day) , from day 28 or day 70 onward; controls receive water only^[2].
Mice^[3]
Tg2576 mice are treated (starting at or after the initiation of plaque pathology) for 2-3 mo with PMX 205 given in the drinking water only (10-20 μg/mL, equivalent to ~3-6 mg/kg/day) or both in drinking water (10-20 μg/mL) and s.c. (1 mg/kg) twice weekly throughout the treatment period. Untreated transgenic animals of same age are used as controls. Nontransgenic littermates are similarly treated or not treated with the drug. 3×Tg mice are also treated with PMX 205 in the drinking water. Due to the low pathology of the males, only female mice of this strain are used for these studies^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (281 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Kosni NN, et al. Expression of complement C5a receptor and the viability of 4T1 tumor cells following agonist-antagonist treatment. J Cancer Res Ther. 2016 Apr-Jun;12(2):590-6. [Content Brief]

[2]. Woodruff TM, et al. The complement factor C5a contributes to pathology in a rat model of amyotrophic lateral sclerosis. J Immunol. 2008 Dec 15;181(12):8727-34. [Content Brief]

[3]. Fonseca MI, et al. Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer's disease. J Immunol. 2009 Jul 15;183(2):1375-83. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.1918 mL	5.9592 mL	11.9184 mL	29.7960 mL
	5 mM	0.2384 mL	1.1918 mL	2.3837 mL	5.9592 mL
	10 mM	0.1192 mL	0.5959 mL	1.1918 mL	2.9796 mL
	15 mM	0.0795 mL	0.3973 mL	0.7946 mL	1.9864 mL
	20 mM	0.0596 mL	0.2980 mL	0.5959 mL	1.4898 mL
	25 mM	0.0477 mL	0.2384 mL	0.4767 mL	1.1918 mL
	30 mM	0.0397 mL	0.1986 mL	0.3973 mL	0.9932 mL
	40 mM	0.0298 mL	0.1490 mL	0.2980 mL	0.7449 mL
	50 mM	0.0238 mL	0.1192 mL	0.2384 mL	0.5959 mL
	60 mM	0.0199 mL	0.0993 mL	0.1986 mL	0.4966 mL
	80 mM	0.0149 mL	0.0745 mL	0.1490 mL	0.3724 mL
	100 mM	0.0119 mL	0.0596 mL	0.1192 mL	0.2980 mL

Keywords

PMX 205

14 Cited Publications

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PMX 205

Immunology/Inflammation Compound Library

Peptide Library

Autoimmune Disease Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Peptide Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) PMX 205

Activité biologique

Chemical Information

Publications (14)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

PMX 205

Immunology/Inflammation Compound Library

Peptide Library

Autoimmune Disease Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Peptide Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) PMX 205

Activité biologique

Chemical Information

Publications (14)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

PMX 205 Related Classifications

HY-110136 Related Classifications